Articles ASAP (As Soon As Publishable)

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November 11, 2009

Corrections to Multidentate Small-Molecule Inhibitors of Vaccinia H1-Related (VHR) Phosphatase Decrease Proliferation of Cervix Cancer Cells

Shuangding Wu, Sofie Vossius, Souad Rahmouni, Ana V. Miletic, Torkel Vang, Jesus Vazquez-Rodriguez, Fabio Cerignoli, Yutaka Arimura, Scott Williams, Tikva Hayes, Michel Moutschen, Stefan Vasile, Maurizio Pellecchia, Tomas Mustelin and Lutz Tautz
Publication Date (Web): November 11, 2009 (Addition/Correction)

Discovery of (Z)-5-(4-Methoxybenzylidene)thiazolidine-2,4-dione, a Readily Available and Orally Active Glitazone for the Treatment of Concanavalin A-Induced Acute Liver Injury of BALB/c Mice

Youfu Luo, Liang Ma, Hao Zheng, Lijuan Chen, Rui Li, Chunmei He, Shengyong Yang, Xia Ye, Zhizhi Chen, Zicheng Li, Yan Gao, Jing Han, Gu He, Li Yang and Yuquan Wei
Publication Date (Web): November 11, 2009 (Article)
DOI: 10.1021/jm901183d

4-Oxo-β-lactams (Azetidine-2,4-diones) Are Potent and Selective Inhibitors of Human Leukocyte Elastase

Jalmira Mulchande, Rudi Oliveira, Marta Carrasco, Lus Gouveia, Rita C. Guedes, Jim Iley and Rui Moreira
Publication Date (Web): November 11, 2009 (Article)

November 10, 2009

Human P2Y14 Receptor Agonists: Truncation of the Hexose Moiety of Uridine-5′-Diphosphoglucose and Its Replacement with Alkyl and Aryl Groups

Arijit Das, Hyojin Ko, Lauren E. Burianek, Matthew O. Barrett, T. Kendall Harden and Kenneth A. Jacobson
Publication Date (Web): November 10, 2009 (Article)
DOI: 10.1021/jm901432g

Corrections to Design, Synthesis, and Biological Evaluation of 6α- and 6β-N-Heterocyclic Substituted Naltrexamine Derivatives as μ Opioid Receptor Selective Antagonists

Guo Li, Lindsey C. Aschenbach, Jianyang Chen, Michael P. Cassidy, David L. Stevens, Bichoy H. Gabra, Dana E. Selley, William L. Dewey, Richard B. Westkaemper and Yan Zhang
Publication Date (Web): November 10, 2009 (Addition/Correction)
DOI: 10.1021/jm9016224

Discovery of 3-Aryl-4-isoxazolecarboxamides as TGR5 Receptor Agonists

Karen A. Evans, Brian W. Budzik, Sean A. Ross, David D. Wisnoski, Jian Jin, Ralph A. Rivero, Mythily Vimal, George R. Szewczyk, Channa Jayawickreme, David L. Moncol, Thomas J. Rimele, Susan L. Armour, Susan P. Weaver, Robert J. Griffin, Sarva M. Tadepalli, Michael R. Jeune, Todd W. Shearer, Zibin B. Chen, Lihong Chen, Donald L. Anderson, J. David Becherer, Maite De Los Frailes and Francisco Javier Colilla
Publication Date (Web): November 10, 2009 (Letter)
DOI: 10.1021/jm901434t

November 9, 2009

Phosphinic Tripeptides as Dual Angiotensin-Converting Enzyme C-Domain and Endothelin-Converting Enzyme-1 Inhibitors

Nicolas Jullien, Anastasios Makritis, Dimitris Georgiadis, Fabrice Beau, Athanasios Yiotakis and Vincent Dive
Publication Date (Web): November 9, 2009 (Article)
DOI: 10.1021/jm9010803

Structural Studies of Pterin-Based Inhibitors of Dihydropteroate Synthase

Kirk E. Hevener, Mi-Kyung Yun, Jianjun Qi, Iain D. Kerr, Kerim Babaoglu, Julian G. Hurdle, Kanya Balakrishna, Stephen W. White and Richard E. Lee
Publication Date (Web): November 9, 2009 (Article)
DOI: 10.1021/jm900861d

November 6, 2009

The Discodermolide Hairpin Structure Flows from Conformationally Stable Modular Motifs

Ashutosh S. Jogalekar, Frederik H. Kriel, Qi Shi, Ben Cornett, Daniel Cicero and James P. Snyder
Publication Date (Web): November 6, 2009 (Article)
DOI: 10.1021/jm9015284

In Vitro and In Vivo Isotope Effects with Hepatitis C Protease Inhibitors: Enhanced Plasma Exposure of Deuterated Telaprevir versus Telaprevir in Rats

Franois Maltais, Young Chun Jung, Minzhang Chen, Jerry Tanoury, Robert B. Perni, Nagraj Mani, Leena Laitinen, Hui Huang, Shengkai Liao, Hongying Gao, Hong Tsao, Eric Block, Chien Ma, Rebecca S. Shawgo, Christopher Town, Christopher L. Brummel, David Howe, S. Pazhanisamy, Scott Raybuck, Mark Namchuk and Youssef L. Bennani
Publication Date (Web): November 6, 2009 (Article)
DOI: 10.1021/jm901023f

Fluorinated Rhodacyanine (SJL-01) Possessing High Efficacy for Visceral Leishmaniasis (VL)

Mei Yang, Chika Arai, Abu Bakar Md., Jun Lu, Jian-Feng Ge, Khanitha Pudhom, Kiyosei Takasu, Kazuki Kasai, Marcel Kaiser, Reto Brun, Vanessa Yardley, Isamu Itoh and Masataka Ihara
Publication Date (Web): November 6, 2009 (Article)
DOI: 10.1021/jm9013086

Design, Synthesis, and Characterization of Peptide-Based Rab Geranylgeranyl Transferase Inhibitors

Kui-Thong Tan, Ester Guiu-Rozas, Robin S. Bon, Zhong Guo, Christine Delon, Stefan Wetzel, Sabine Arndt, Kirill Alexandrov, Herbert Waldmann, Roger S. Goody, Yao-Wen Wu and Wulf Blankenfeldt
Publication Date (Web): November 6, 2009 (Article)
DOI: 10.1021/jm901117d

N-Sulfonylanthranilic Acid Derivatives as Allosteric Inhibitors of Dengue Viral RNA-Dependent RNA Polymerase

Zheng Yin, Yen-Liang Chen, Ravinder Reddy Kondreddi, Wai Ling Chan, Gang Wang, Ru Hui Ng, Joanne Y. H. Lim, Wan Yen Lee, Duraiswamy A. Jeyaraj, Pornwaratt Niyomrattanakit, Daying Wen, Alex Chao, J. Fraser Glickman, Hans Voshol, Dieter Mueller, Carsten Spanka, Sigmar Dressler, Shahul Nilar, Subhash G. Vasudevan, Pei-Yong Shi and Thomas H. Keller
Publication Date (Web): November 6, 2009 (Letter)
DOI: 10.1021/jm901044z

Discovery of 4-Morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as Highly Potent and Selective ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin (mTOR): Optimization of the 6-Aryl Substituent

Jeroen C. Verheijen, David J. Richard, Kevin Curran, Joshua Kaplan, Mark Lefever, Pawel Nowak, David J. Malwitz, Natasja Brooijmans, Lourdes Toral-Barza, Wei-Guo Zhang, Judy Lucas, Irwin Hollander, Semiramis Ayral-Kaloustian, Tarek S. Mansour, Ker Yu and Arie Zask
Publication Date (Web): November 6, 2009 (Article)
DOI: 10.1021/jm9013828

Design, Synthesis, and Biological Evaluations of 2,5-Diaryl-2,3-dihydro-1,3,4-oxadiazoline Analogs of Combretastatin-A4

Lauren Lee, Lyda M. Robb, Megan Lee, Ryan Davis, Hilary Mackay, Sameer Chavda, Balaji Babu, Erin L. O’Brien, April L. Risinger, Susan L. Mooberry and Moses Lee
Publication Date (Web): November 6, 2009 (Article)
DOI: 10.1021/jm901268n

November 5, 2009

Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a

Feng Liu, Xin Chen, Abdellah Allali-Hassani, Amy M. Quinn, Gregory A. Wasney, Aiping Dong, Dalia Barsyte, Ivona Kozieradzki, Guillermo Senisterra, Irene Chau, Alena Siarheyeva, Dmitri B. Kireev, Ajit Jadhav, J. Martin Herold, Stephen V. Frye, Cheryl H. Arrowsmith, Peter J. Brown, Anton Simeonov, Masoud Vedadi and Jian Jin
Publication Date (Web): November 5, 2009 (Letter)
DOI: 10.1021/jm901543m

1,2,4-Triazolyl Azabicyclo[3.1.0]hexanes: A New Series of Potent and Selective Dopamine D3 Receptor Antagonists

Fabrizio Micheli, Luca Arista, Giorgio Bonanomi, Frank E. Blaney, Simone Braggio, Anna Maria Capelli, Anna Checchia, Federica Damiani, Romano Di-Fabio, Stefano Fontana, Gabriella Gentile, Cristiana Griffante, Dieter Hamprecht, Carla Marchioro, Manolo Mugnaini, Jacqui Piner, Emiliangelo Ratti, Giovanna Tedesco, Luca Tarsi, Silvia Terreni, Angela Worby, Charles R. Ashby, Jr. and Christian Heidbreder
Publication Date (Web): November 5, 2009 (Article)
DOI: 10.1021/jm901319p

Discovery of trans-4-[1-[[2,5-Dichloro-4-(1-methyl-3-indolylcarboxamido)phenyl]acetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic Acid: An Orally Active, Selective Very Late Antigen-4 Antagonist

Fumihito Muro, Shin Iimura, Yuuichi Sugimoto, Yoshiyuki Yoneda, Jun Chiba, Toshiyuki Watanabe, Masaki Setoguchi, Yutaka Iigou, Keiko Matsumoto, Atsushi Satoh, Gensuke Takayama, Tomoe Taira, Mika Yokoyama, Tohru Takashi, Atsushi Nakayama and Nobuo Machinaga
Publication Date (Web): November 5, 2009 (Article)

Poly-N-methylated Amyloid β-Peptide (Aβ) C-Terminal Fragments Reduce Aβ Toxicity in Vitro and in Drosophila melanogaster

Partha Pratim Bose, Urmimala Chatterjee, Charlotte Nerelius, Thavendran Govender, Thomas Norstrm, Adolf Gogoll, Anna Sandegren, Emmanuelle Gthelid, Jan Johansson and Per I. Arvidsson
Publication Date (Web): November 5, 2009 (Article)

Drug Effects Viewed from a Signal Transduction Network Perspective

Anton F. Fliri, William T. Loging and Robert A. Volkmann
Publication Date (Web): November 5, 2009 (Article)
DOI: 10.1021/jm901001p

November 3, 2009

Binding Ensemble Profiling with Photoaffinity Labeling (BEProFL) Approach: Mapping the Binding Poses of HDAC8 Inhibitors

Bai He, Subash Velaparthi, Gilles Pieffet, Chris Pennington, Aruna Mahesh, Denise L. Holzle, Michael Brunsteiner, Richard van Breemen, Sylvie Y. Blond and Pavel A. Petukhov
Publication Date (Web): November 3, 2009 (Article)
DOI: 10.1021/jm9005077

Might Adrenergic α2C-Agonists/α2A-Antagonists Become Novel Therapeutic Tools for Pain Treatment with Morphine?

Claudia Cardinaletti, Laura Mattioli, Francesca Ghelfi, Fabio Del Bello, Mario Giannella, Ariana Bruzzone, Herv Paris, Marina Perfumi, Alessandro Piergentili, Wilma Quaglia and Maria Pigini
Publication Date (Web): November 3, 2009 (Brief Article)
DOI: 10.1021/jm901262f

November 2, 2009

Biaryl Ethers as Novel Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Key Mutant Viruses

Dai-Shi Su, John J. Lim, Elizabeth Tinney, Bang-Lin Wan, Mary Beth Young, Kenneth D. Anderson, Deanne Rudd, Vandna Munshi, Carolyn Bahnck, Peter J. Felock, Meiquing Lu, Ming-Tain Lai, Sinoeun Touch, Gregory Moyer, Daniel J DiStefano, Jessica A. Flynn, Yuexia Liang, Rosa Sanchez, Rebecca Perlow-Poehnelt, Mike Miller, Joe P. Vacca, Theresa M. Williams and Neville J. Anthony
Publication Date (Web): November 2, 2009 (Article)
DOI: 10.1021/jm901230r

The Role of Membranes in the Organization of HIV-1 Gag p6 and Vpr: p6 Shows High Affinity for Membrane Bilayers Which Substantially Increases the Interaction between p6 and Vpr.

Gilmar F. Salgado, Alexander Vogel, Rodrigue Marquant, Scott E. Feller, Serge Bouaziz and Isabel D. Alves
Publication Date (Web): November 2, 2009 (Article)
DOI: 10.1021/jm901106t

4-Pregnen-21-ol-3,20-dione-21-(4-bromobenzenesufonate) (NSC 88915) and Related Novel Steroid Derivatives as Tyrosyl-DNA Phosphodiesterase (Tdp1) Inhibitors

Thomas S. Dexheimer, Lalji K. Gediya, Andrew G. Stephen, Iwona Weidlich, Smitha Antony, Christophe Marchand, Heidrun Interthal, Marc Nicklaus, Robert J. Fisher, Vincent C. Njar and Yves Pommier
Publication Date (Web): November 2, 2009 (Article)
DOI: 10.1021/jm901061s

Discovery of Novel Benzoxazinones as Potent and Orally Active Long Chain Fatty Acid Elongase 6 Inhibitors

Takashi Mizutani, Shiho Ishikawa, Tsuyoshi Nagase, Hidekazu Takahashi, Takashi Fujimura, Takahide Sasaki, Akira Nagumo, Ken Shimamura, Yasuhisa Miyamoto, Hidefumi Kitazawa, Maki Kanesaka, Ryo Yoshimoto, Katsumi Aragane, Shigeru Tokita and Nagaaki Sato
Publication Date (Web): November 2, 2009 (Article)
DOI: 10.1021/jm900915x

Structure−Activity Relationship Studies of Chalcone Leading to 3-Hydroxy-4,3′,4′,5′-tetramethoxychalcone and Its Analogues as Potent Nuclear Factor κB Inhibitors and Their Anticancer Activities

Balasubramanian Srinivasan, Thomas E. Johnson, Rahul Lad and Chengguo Xing
Publication Date (Web): November 2, 2009 (Article)
DOI: 10.1021/jm901278z

Bis(dialkylaminethiocarbonyl)disulfides as Potent and Selective Monoglyceride Lipase Inhibitors

Coco N. Kapanda, Giulio G. Muccioli, Geoffray Labar, Jacques H. Poupaert and Didier M. Lambert
Publication Date (Web): November 2, 2009 (Brief Article)
DOI: 10.1021/jm901323s

October 30, 2009

Exploring Chemical Space with Aptamers

Michael Famulok
Publication Date (Web): October 30, 2009 (Perspective)
DOI: 10.1021/jm9014789

Microtubule-Stabilizing Activity of Zampanolide, a Potent Macrolide Isolated from the Tongan Marine Sponge Cacospongia mycofijiensis

Jessica J. Field, A. Jonathan Singh, Arun Kanakkanthara, Tu’ikolongahau Halafihi, Peter T. Northcote and John H. Miller
Publication Date (Web): October 30, 2009 (Brief Article)
DOI: 10.1021/jm901249g

Synthesis and Evaluation of Antiallodynic and Anticonvulsant Activity of Novel Amide and Urea Derivatives of Valproic Acid Analogues

Dan Kaufmann, Meir Bialer, Jakob Avi Shimshoni, Marshall Devor and Boris Yagen
Publication Date (Web): October 30, 2009 (Article)
DOI: 10.1021/jm901229s

Synthetic mRNA Splicing Modulator Compounds with in Vivo Antitumor Activity

Chandraiah Lagisetti, Alan Pourpak, Tinopiwa Goronga, Qin Jiang, Xiaoli Cui, Judith Hyle, Jill M. Lahti, Stephan W. Morris and Thomas R. Webb
Publication Date (Web): October 30, 2009 (Article)
DOI: 10.1021/jm901215m

Hypoxia-Activated Prodrugs: Substituent Effects on the Properties of Nitro seco-1,2,9,9a-Tetrahydrocyclopropa[c]benz[e]indol-4-one (nitroCBI) Prodrugs of DNA Minor Groove Alkylating Agents

Moana Tercel, Graham J. Atwell, Shangjin Yang, Ralph J. Stevenson, K. Jane Botting, Maruta Boyd, Eileen Smith, Robert F. Anderson, William A. Denny, William R. Wilson and Frederik B. Pruijn
Publication Date (Web): October 30, 2009 (Article)
DOI: 10.1021/jm901202b

Synthesis and Evaluation of Three 18F-Labeled Aminophenylbenzothiazoles as Amyloid Imaging Agents

Kim Serdons, Koen Van Laere, Peter Janssen, Hank F. Kung, Guy Bormans and Alfons Verbruggen
Publication Date (Web): October 30, 2009 (Article)
DOI: 10.1021/jm900871v

Identification of Death-Associated Protein Kinases Inhibitors Using Structure-Based Virtual Screening

Masako Okamoto, Kiyoshi Takayama, Tomoko Shimizu, Kazuhiro Ishida, Osamu Takahashi and Toshio Furuya
Publication Date (Web): October 30, 2009 (Brief Article)
DOI: 10.1021/jm901191q

Carborane Derivatives Loaded into Liposomes as Efficient Delivery Systems for Boron Neutron Capture Therapy

S. Altieri, M. Balzi, S. Bortolussi, P. Bruschi, L. Ciani, A. M. Clerici, P. Faraoni, C. Ferrari, M. A. Gadan, L. Panza, D. Pietrangeli, G. Ricciardi and S. Ristori
Publication Date (Web): October 30, 2009 (Article)
DOI: 10.1021/jm900763b

Synthesis and Biological Evaluation of Coumarin-Based Inhibitors of NAD(P)H: Quinone Oxidoreductase-1 (NQO1)

Karen A. Nolan, Jeremy R. Doncaster, Mark S. Dunstan, Katherine A. Scott, A. David Frenkel, David Siegel, David Ross, John Barnes, Colin Levy, David Leys, Roger C. Whitehead, Ian J. Stratford and Richard A. Bryce
Publication Date (Web): October 30, 2009 (Article)
DOI: 10.1021/jm9011609

β-Lactams Derived from a Carbapenem Chiron Are Selective Inhibitors of Human Fatty Acid Amide Hydrolase versus Human Monoacylglycerol Lipase

Marion Feledziak, Catherine Michaux, Allan Urbach, Geoffray Labar, Giulio G. Muccioli, Didier M. Lambert and Jacqueline Marchand-Brynaert
Publication Date (Web): October 30, 2009 (Article)
DOI: 10.1021/jm9008532

October 29, 2009

Design of HIV Protease Inhibitors Based on Inorganic Polyhedral Metallacarboranes

Pavlna ezov, Jana Pokorn, Ji Brynda, Milan Koek, Petr Cgler, Martin Lepk, Jindich Fanfrlk, Jan ez, Klra Grantz akov, Irena Sieglov, Jaromr Pleek, Vclav cha, Bohumr Grner, Heike Oberwinkler, Juraj Sedlek’, Hans-Georg Krusslich, Pavel Hobza, Vladimr Krl and Jan Konvalinka
Publication Date (Web): October 29, 2009 (Article)
DOI: 10.1021/jm9011388

Structure−Activity Relationships of Polymyxin Antibiotics

Tony Velkov, Philip E. Thompson, Roger L. Nation and Jian Li
Publication Date (Web): October 29, 2009 (Perspective)
DOI: 10.1021/jm900999h

Discovery of 2-{4-[(3S)-Piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): A Novel Oral Poly(ADP-ribose)polymerase (PARP) Inhibitor Efficacious in BRCA-1 and -2 Mutant Tumors

Philip Jones, Sergio Altamura, Julia Boueres, Federica Ferrigno, Massimiliano Fonsi, Claudia Giomini, Stefania Lamartina, Edith Monteagudo, Jesus M. Ontoria, Maria Vittoria Orsale, Maria Cecilia Palumbi, Silvia Pesci, Giuseppe Roscilli, Rita Scarpelli, Carsten Schultz-Fademrecht, Carlo Toniatti and Michael Rowley
Publication Date (Web): October 29, 2009 (Article)
DOI: 10.1021/jm901188v

The Synthesis of Haptens and Their Use for the Development of Monoclonal Antibodies for Treating Methamphetamine Abuse

F. Ivy Carroll, Philip Abraham, Paul K. Gong, Ramakrishna R. Pidaparthi, Bruce E. Blough, Yingni Che, Amber Hampton, Melinda Gunnell, Jackson O. Lay, Jr., Eric C. Peterson and S. Michael Owens
Publication Date (Web): October 29, 2009 (Article)
DOI: 10.1021/jm901134w

Asymmetrical Diaromatic Guanidinium/2-Aminoimidazolinium Derivatives: Synthesis and DNA Affinity

Padraic S. Nagle, Fernando Rodriguez, Amila Kahvedi, Susan J. Quinn and Isabel Rozas
Publication Date (Web): October 29, 2009 (Article)
DOI: 10.1021/jm901017t

Azaindole Hydroxamic Acids are Potent HIV-1 Integrase Inhibitors

Michael B. Plewe, Scott L. Butler, Klaus R. Dress, Qiyue Hu, Ted W. Johnson, Jon E. Kuehler, Atsuo Kuki, Hieu Lam, Wen Liu, Dawn Nowlin, Qinghai Peng, Sadayappan V. Rahavendran, Steven P. Tanis, Khanh T. Tran, Hai Wang, Anle Yang and Junhu Zhang
Publication Date (Web): October 29, 2009 (Article)
DOI: 10.1021/jm900862n

October 28, 2009

Inhibitors for Human Glutaminyl Cyclase by Structure Based Design and Bioisosteric Replacement

Mirko Buchholz, Antje Hamann, Susanne Aust, Wolfgang Brandt, Livia Bhme, Torsten Hoffmann, Stephan Schilling, Hans-Ulrich Demuth and Ulrich Heiser
Publication Date (Web): October 28, 2009 (Article)
DOI: 10.1021/jm900969p

Novel Compounds Designed as Antistress Agents

Karyophyllis C. Tsiakitzis, Eleni A. Rekka, Angeliki P. Kourounakis and Panos N. Kourounakis
Publication Date (Web): October 28, 2009 (Brief Article)
DOI: 10.1021/jm901169b

Losartan-Antioxidant Hybrids: Novel Molecules for the Prevention of Hypertension-Induced Cardiovascular Damage

Gonzalo Garca, Manuel Rodrguez-Puyol, Ramn Alajarn, Isabel Serrano, Patricia Snchez-Alonso, Mercedes Griera, Juan J. Vaquero, Diego Rodrguez-Puyol, Julio lvarez-Builla and Mara L. Dez-Marqus
Publication Date (Web): October 28, 2009 (Article)
DOI: 10.1021/jm9003957

From Serendipity to Rational Antituberculosis Drug Discovery of Mefloquine-Isoxazole Carboxylic Acid Esters

Jialin Mao, Hai Yuan, Yuehong Wang, Baojie Wan, Marco Pieroni, Qingqing Huang, Richard B. van Breemen, Alan P. Kozikowski and Scott G. Franzblau
Publication Date (Web): October 28, 2009 (Article)
DOI: 10.1021/jm900340a

October 27, 2009

Synthesis, Crystallization, and Biological Evaluation of an Orally Active Prodrug of Gemcitabine

David M. Bender, Jingqi Bao, Anne H. Dantzig, William D. Diseroad, Kevin L. Law, Nicholas A. Magnus, Jeffrey A. Peterson, Everett J. Perkins, Yangwei J. Pu, Susan M. Reutzel-Edens, David M. Remick, James J. Starling, Gregory A. Stephenson, Radhe K. Vaid, Deyi Zhang and James R. McCarthy
Publication Date (Web): October 27, 2009 (Letter)
DOI: 10.1021/jm901181h

Selectively Nonselective Kinase Inhibition: Striking the Right Balance

Richard Morphy
Publication Date (Web): October 27, 2009 (Perspective)
DOI: 10.1021/jm901132v

αvβ3 Integrin-Targeting Arg-Gly-Asp (RGD) Peptidomimetics Containing Oligoethylene Glycol (OEG) Spacers

Vincent Rerat, Georges Dive, Alex A. Cordi, Gordon C. Tucker, Reine Bareille, Jolle Amde, Laurence Bordenave and Jacqueline Marchand-Brynaert
Publication Date (Web): October 27, 2009 (Article)
DOI: 10.1021/jm901133z

χ-Conopeptide Pharmacophore Development: Toward a Novel Class of Norepinephrine Transporter Inhibitor (Xen2174) for Pain

Andreas Brust, Elka Palant, Daniel E. Croker, Barbara Colless, Roger Drinkwater, Brad Patterson, Christina I. Schroeder, David Wilson, Carsten K. Nielsen, Maree T. Smith, Dianne Alewood, Paul F. Alewood and Richard J. Lewis
Publication Date (Web): October 27, 2009 (Article)
DOI: 10.1021/jm9003413

Highlights in the Discovery of Antiviral Drugs: A Personal Retrospective

Erik De Clercq
Publication Date (Web): October 27, 2009 (Perspective)
DOI: 10.1021/jm900932g

A Novel Manganese Complex Effective as Superoxide Anion Scavenger and Therapeutic Agent against Cell and Tissue Oxidative Injury

Paola Failli, Daniele Bani, Andrea Bencini, Miriam Cantore, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Claudia Giorgi, Massimo Innocenti, Francesco Rugi, Alessio Spepi, Roberto Udisti and Barbara Valtancoli
Publication Date (Web): October 27, 2009 (Article)
DOI: 10.1021/jm901298x

Reactivity of 6-Halopurine Analogs with Glutathione as a Radiotracer for Assessing Function of Multidrug Resistance-Associated Protein 1

Toshimitsu Okamura, Tatsuya Kikuchi, Kiyoshi Fukushi and Toshiaki Irie
Publication Date (Web): October 27, 2009 (Article)
DOI: 10.1021/jm901332c

October 26, 2009

(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: A Wingless β-Catenin Agonist That Increases Bone Formation Rate

Jeffrey C. Pelletier, Joseph T. Lundquist, IV, Adam M. Gilbert, Nipa Alon, Frederick J. Bex, Bheem M. Bhat, Mattew G. Bursavich, Valerie E. Coleburn, Luciana A. Felix, Daniel M. Green, Paula Green, Diane B. Hauze, Yogendra P. Kharode, Ho-Sun Lam, Susan R. Lockhead, Ronald L. Magolda, Jeanne J. Matteo, John F. Mehlmann, Colleen Milligan, Richard J. Murrills, Jennifer Pirrello, Sally Selim, Michael C. Sharp, Ray J. Unwalla, Matthew D. Vera, Jay E. Wrobel, Paul Yaworsky and Peter V. N. Bodine
Publication Date (Web): October 26, 2009 (Letter)
DOI: 10.1021/jm9014197

Neuroprotective and Cholinergic Properties of Multifunctional Glutamic Acid Derivatives for the Treatment of Alzheimer’s Disease

Mariana P. Arce, Mara Isabel Rodrguez-Franco, Gema C. Gonzlez-Muoz, Concepcin Prez, Beatriz Lpez, Mercedes Villarroya, Manuela G. Lpez, Antonio G. Garca and Santiago Conde
Publication Date (Web): October 26, 2009 (Article)
DOI: 10.1021/jm900628z

Synthesis, Structure−Activity Relationships, and Characterization of Novel Nonsteroidal and Selective Androgen Receptor Modulators

Nathalie Schlienger, Birgitte W. Lund, Jan Pawlas, Fabrizio Badalassi, Fabio Bertozzi, Rasmus Lewinsky, Alma Fejzic, Mikkel B. Thygesen, Ali Tabatabaei, Stefania Risso Bradley, Luis R. Gardell, Fabrice Piu and Roger Olsson
Publication Date (Web): October 26, 2009 (Article)
DOI: 10.1021/jm901149c

Discovery and Optimization of Chromenotriazolopyrimidines as Potent Inhibitors of the Mouse Double Minute 2−Tumor Protein 53 Protein−Protein Interaction

John G. Allen, Matthew P. Bourbeau, G. Erich Wohlhieter, Michael D. Bartberger, Klaus Michelsen, Randall Hungate, Robert C. Gadwood, Rick D. Gaston, Bruce Evans, Larry W. Mann, Michael E. Matison, Stephen Schneider, Xin Huang, Dongyin Yu, Paul S. Andrews, Andreas Reichelt, Alexander M. Long, Peter Yakowec, Evelyn Y. Yang, Tani Ann Lee and Jonathan D. Oliner
Publication Date (Web): October 26, 2009 (Article)
DOI: 10.1021/jm900681h

Novel Macrocyclic Inhibitors of Hepatitis C NS3/4A Protease Featuring a 2-Amino-1,3-thiazole as a P4 Carbamate Replacement

M. Emilia Di Francesco, Gabriella Dessole, Emanuela Nizi, Paola Pace, Uwe Koch, Fabrizio Fiore, Silvia Pesci, Jillian Di Muzio, Edith Monteagudo, Michael Rowley and Vincenzo Summa
Publication Date (Web): October 26, 2009 (Article)
DOI: 10.1021/jm900524b

October 21, 2009

18F Stilbenes and Styrylpyridines for PET Imaging of Aβ Plaques in Alzheimer’s Disease: A Miniperspective

Hank F. Kung, Seok Rye Choi, Wenchao Qu, Wei Zhang and Daniel Skovronsky
Publication Date (Web): October 21, 2009 (Perspective)
DOI: 10.1021/jm901039z

October 20, 2009

Design, Synthesis, and Structure−Activity Relationship of Indole-3-glyoxylamide Libraries Possessing Highly Potent Activity in a Cell Line Model of Prion Disease

Mark J. Thompson, Vinciane Borsenberger, Jennifer C. Louth, Katie E. Judd and Beining Chen
Publication Date (Web): October 20, 2009 (Article)

Exploring the Importance of Piperazine N-Atoms for σ2 Receptor Affinity and Activity in a Series of Analogs of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28)

Francesco Berardi, Carmen Abate, Savina Ferorelli, Vincenzo Uricchio, Nicola A. Colabufo, Mauro Niso and Roberto Perrone
Publication Date (Web): October 20, 2009 (Article)
DOI: 10.1021/jm9007505

October 19, 2009

Discovery of Potent and Selective Inhibitors of the Mammalian Target of Rapamycin (mTOR) Kinase

Pawel Nowak, Derek C. Cole, Natasja Brooijmans, Matthew G. Bursavich, Kevin J. Curran, John W. Ellingboe, James J. Gibbons, Irwin Hollander, YongBo Hu, Joshua Kaplan, David J. Malwitz, Lourdes Toral-Barza, Jeroen C. Verheijen, Arie Zask, Wei-Guo Zhang and Ker Yu
Publication Date (Web): October 19, 2009 (Article)
DOI: 10.1021/jm9012642

Synthesis and Biological Evaluation of 2-Alkynyl-N6-methyl-5′-N-methylcarboxamidoadenosine Derivatives as Potent and Highly Selective Agonists for the Human Adenosine A3 Receptor

Rosaria Volpini, Michela Buccioni, Diego Dal Ben, Catia Lambertucci, Carmen Lammi, Gabriella Marucci, Anna T. Ramadori, Karl-Norbert Klotz and Gloria Cristalli
Publication Date (Web): October 19, 2009 (Brief Article)
DOI: 10.1021/jm900754g

October 15, 2009

Three-Dimensional Pharmacophore Methods in Drug Discovery

Andrew R. Leach, Valerie J. Gillet, Richard A. Lewis and Robin Taylor
Publication Date (Web): October 15, 2009 (Perspective)
DOI: 10.1021/jm900817u

October 9, 2009

Identification of a Critical Residue in the Transmembrane Domain 2 of Tachykinin Neurokinin 3 Receptor Affecting the Dissociation Kinetics and Antagonism Mode of Osanetant (SR 142801) and Piperidine-Based Structures

Pari Malherbe, Claudia Kratzeisen, Anne Marcuz, Marie-Thrse Zenner, Matthias H. Nettekoven, Hasane Ratni, Joseph G. Wettstein and Caterina Bissantz
Publication Date (Web): October 9, 2009 (Article)
DOI: 10.1021/jm900948q

October 8, 2009

Toward a Rational Design of Multitarget-Directed Antioxidants: Merging Memoquin and Lipoic Acid Molecular Frameworks

Maria Laura Bolognesi, Andrea Cavalli, Christian Bergamini, Romana Fato, Giorgio Lenaz, Michela Rosini, Manuela Bartolini, Vincenza Andrisano and Carlo Melchiorre
Publication Date (Web): October 8, 2009 (Brief Article)
DOI: 10.1021/jm901123n

October 5, 2009

Scope and Difficulty in Generating Theoretical Insights Regarding Ligand Recognition and Activation of the β2 Adrenergic Receptor

Marvin A. Soriano-Ursa, Jos G. Trujillo-Ferrara and Jos Correa-Basurto
Publication Date (Web): October 5, 2009 (Perspective)
DOI: 10.1021/jm900419a

October 2, 2009

Imidazoquines as Antimalarial and Antipneumocystis Agents

Nuno Vale, Miguel Prudncio, Catarina A. Marques, Margaret S. Collins, Jiri Gut, Ftima Nogueira, Joana Matos, Philip J. Rosenthal, Melanie T. Cushion, Virglio E. do Rosrio, Maria M. Mota, Rui Moreira and Paula Gomes
Publication Date (Web): October 2, 2009 (Article)
DOI: 10.1021/jm900738c

September 30, 2009

Amide Linkage Isomerism As an Activity Switch for Organometallic Osmium and Ruthenium Anticancer Complexes

Sabine H. van Rijt, Andrew J. Hebden, Thakshila Amaresekera, Robert J. Deeth, Guy J. Clarkson, Simon Parsons, Patrick C. McGowan and Peter J. Sadler
Publication Date (Web): September 30, 2009 (Article)
DOI: 10.1021/jm900731j

September 29, 2009

Pentapeptides Displaying μ Opioid Receptor Agonist and δ Opioid Receptor Partial Agonist/Antagonist Properties

Lauren C. Purington, Irina D. Pogozheva, John R. Traynor and Henry I. Mosberg
Publication Date (Web): September 29, 2009 (Article)
DOI: 10.1021/jm9007483

Further Studies on Arylpiperazinyl Alkyl Pyridazinones: Discovery of an Exceptionally Potent, Orally Active, Antinociceptive Agent in Thermally Induced Pain

Claudio Biancalani, Maria Paola Giovannoni, Stefano Pieretti, Nicoletta Cesari, Alessia Graziano, Claudia Vergelli, Agostino Cilibrizzi, Amalia Di Gianuario, Mariantonella Colucci, Giorgina Mangano, Beatrice Garrone, Lorenzo Polenzani and Vittorio Dal Piaz
Publication Date (Web): September 29, 2009 (Article)
DOI: 10.1021/jm900458r

September 28, 2009

Twenty-Six Years of Anti-HIV Drug Discovery: Where Do We Stand and Where Do We Go?

Youcef Mehellou and Erik De Clercq
Publication Date (Web): September 28, 2009 (Perspective)
DOI: 10.1021/jm900492g

September 24, 2009

Discovery of a 2,4-Disubstituted Pyrrolo[1,2-f][1,2,4]triazine Inhibitor (BMS-754807) of Insulin-like Growth Factor Receptor (IGF-1R) Kinase in Clinical Development

Mark D. Wittman, Joan M. Carboni, Zheng Yang, Francis Y. Lee, Melissa Antman, Ricardo Attar, Praveen Balimane, Chiehying Chang, Cliff Chen, Lorell Discenza, David Frennesson, Marco M. Gottardis, Ann Greer, Warren Hurlburt, Walter Johnson, David R. Langley, Aixin Li, Jianqing Li, Peiying Liu, Harold Mastalerz, Arvind Mathur, Krista Menard, Karishma Patel, John Sack, Xiaopeng Sang, Mark Saulnier, Daniel Smith, Kevin Stefanski, George Trainor, Upender Velaparthi, Guifen Zhang, Kurt Zimmermann and Dolatrai M. Vyas
Publication Date (Web): September 24, 2009 (Letter)
DOI: 10.1021/jm900786r

September 23, 2009

Discovery of Azetidinyl Ketolides for the Treatment of Susceptible and Multidrug Resistant Community-Acquired Respiratory Tract Infections

Thomas V. Magee, Sharon L. Ripp, Bryan Li, Richard A. Buzon, Lou Chupak, Thomas J. Dougherty, Steven M. Finegan, Dennis Girard, Anne E. Hagen, Michael J. Falcone, Kathleen A. Farley, Karl Granskog, Joel R. Hardink, Michael D. Huband, Barbara J. Kamicker, Takushi Kaneko, Michael J. Knickerbocker, Jennifer L. Liras, Andrea Marra, Ivy Medina, Thuy-Trinh Nguyen, Mark C. Noe, R. Scott Obach, John P. O’Donnell, Joseph B. Penzien, Usa Datta Reilly, John R. Schafer, Yue Shen, Gregory G. Stone, Timothy J. Strelevitz, Jianmin Sun, Amelia Tait-Kamradt, Alfin D. N. Vaz, David A. Whipple, Daniel W. Widlicka, Donn G. Wishka, Joanna P. Wolkowski and Mark E. Flanagan
Publication Date (Web): September 23, 2009 (Article)
DOI: 10.1021/jm900729s

September 22, 2009

Synthesis of New Alkylaminooxysterols with Potent Cell Differentiating Activities: Identification of Leads for the Treatment of Cancer and Neurodegenerative Diseases

Philippe de Medina, Michael R. Paillasse, Bruno Payr, Sandrine Silvente-Poirot and Marc Poirot
Publication Date (Web): September 22, 2009 (Article)
DOI: 10.1021/jm901063e

Potent and Selective Steroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 7, an Enzyme That Catalyzes the Reduction of the Key Hormones Estrone and Dihydrotestosterone

dith Bellavance, Van Luu-The and Donald Poirier
Publication Date (Web): September 22, 2009 (Article)
DOI: 10.1021/jm900921c

September 21, 2009

Inhibitors of Human Immunodeficiency Virus Type 1 (HIV-1) Attachment. 5. An Evolution from Indole to Azaindoles Leading to the Discovery of 1-(4-Benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a Drug Candidate That Demonstrates Antiviral Activity in HIV-1-Infected Subjects

Tao Wang, Zhiwei Yin, Zhongxing Zhang, John A. Bender, Zhong Yang, Graham Johnson, Zheng Yang, Lisa M. Zadjura, Celia J. D’Arienzo, Dawn DiGiugno Parker, Christophe Gesenberg, Gregory A. Yamanaka, Yi-Fei Gong, Hsu-Tso Ho, Hua Fang, Nannan Zhou, Brian V. McAuliffe, Betsy J. Eggers, Li Fan, Beata Nowicka-Sans, Ira B. Dicker, Qi Gao, Richard J. Colonno, Pin-Fang Lin, Nicholas A. Meanwell and John F. Kadow
Publication Date (Web): September 21, 2009 (Article)
DOI: 10.1021/jm900843g

September 16, 2009

Design, Synthesis, and Biological Evaluation of Substituted Naphthalene Imides and Diimides as Anticancer Agent

Vincenzo Tumiatti, Andrea Milelli, Anna Minarini, Marialuisa Micco, Anna Gasperi Campani, Laura Roncuzzi, Daniela Baiocchi, Jessica Marinello, Giovanni Capranico, Maddalena Zini, Claudio Stefanelli and Carlo Melchiorre
Publication Date (Web): September 16, 2009 (Brief Article)
DOI: 10.1021/jm901131m

Mechanistic Insight into the Inhibition of Matrix Metalloproteinases by Platinum Substrates

Fabio Arnesano, Angela Boccarelli, Daniele Cornacchia, Fiorentin Nushi, Rossella Sasanelli, Mauro Coluccia and Giovanni Natile
Publication Date (Web): September 16, 2009 (Article)
DOI: 10.1021/jm900845t

Heat Shock Protein 90: Inhibitors in Clinical Trials

Marco A. Biamonte, Ryan Van de Water, Joseph W. Arndt, Robert H. Scannevin, Daniel Perret and Wen-Cherng Lee
Publication Date (Web): September 16, 2009 (Perspective)
DOI: 10.1021/jm9004708

Identification of N-(5-tert-Butyl-isoxazol-3-yl)-N′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea Dihydrochloride (AC220), a Uniquely Potent, Selective, and Efficacious FMS-Like Tyrosine Kinase-3 (FLT3) Inhibitor

Qi Chao, Kelly G. Sprankle, Robert M. Grotzfeld, Andiliy G. Lai, Todd A. Carter, Anne Marie Velasco, Ruwanthi N. Gunawardane, Merryl D. Cramer, Michael F. Gardner, Joyce James, Patrick P. Zarrinkar, Hitesh K. Patel and Shripad S. Bhagwat
Publication Date (Web): September 16, 2009 (Article)
DOI: 10.1021/jm9007533

September 11, 2009

Design, Synthesis, and Structure−Activity Relationship of a Novel Series of 2-Aryl 5-(4-Oxo-3-phenethyl-2-thioxothiazolidinylidenemethyl)furans as HIV-1 Entry Inhibitors

Alan R. Katritzky, Srinivasa R. Tala, Hong Lu, Anatoliy V. Vakulenko, Qi-Yin Chen, Jothilingam Sivapackiam, Keyur Pandya, Shibo Jiang and Asim K. Debnath
Publication Date (Web): September 11, 2009 (Article)
DOI: 10.1021/jm900450n

Design, Synthesis, Protein−Ligand X-ray Structure, and Biological Evaluation of a Series of Novel Macrocyclic Human Immunodeficiency Virus-1 Protease Inhibitors to Combat Drug Resistance

Arun K. Ghosh, Sarang Kulkarni, David D. Anderson, Lin Hong, Abigail Baldridge, Yuan-Fang Wang, Alexander A. Chumanevich, Andrey Y. Kovalevsky, Yasushi Tojo, Masayuki Amano, Yasuhiro Koh, Jordan Tang, Irene T. Weber and Hiroaki Mitsuya
Publication Date (Web): September 11, 2009 (Article)
DOI: 10.1021/jm900695w

September 10, 2009

Foreword: American Chemical Society Division of Medicinal Chemistry. Celebrating 100 Years of Excellence

Patrick M. Woster
Publication Date (Web): September 10, 2009 (Perspective)
DOI: 10.1021/jm901089d

2-Phenylpyrazolo[4,3-d]pyrimidin-7-one as a New Scaffold To Obtain Potent and Selective Human A3 Adenosine Receptor Antagonists: New Insights into the Receptor−Antagonist Recognition

Ombretta Lenzi, Vittoria Colotta, Daniela Catarzi, Flavia Varano, Daniela Poli, Guido Filacchioni, Katia Varani, Fabrizio Vincenzi, Pier Andrea Borea, Silvia Paoletta, Erika Morizzo and Stefano Moro
Publication Date (Web): September 10, 2009 (Article)
DOI: 10.1021/jm900718w

September 9, 2009

The Medicinal Chemistry of Dengue Fever

Andrew J. Stevens, Michelle E. Gahan, Suresh Mahalingam and Paul A. Keller
Publication Date (Web): September 9, 2009 (Perspective)
DOI: 10.1021/jm900652e

September 8, 2009

Rapid Generation of a High Quality Lead for Transforming Growth Factor-β (TGF-β) Type I Receptor (ALK5)

Frederick W. Goldberg, Richard A. Ward, Steven J. Powell, Judit . Debreczeni, Richard A. Norman, Nicola J. Roberts, Allan P. Dishington, Helen J. Gingell, Kate F. Wickson and Andrew L. Roberts
Publication Date (Web): September 8, 2009 (Brief Article)
DOI: 10.1021/jm900807w

September 4, 2009

Nonpeptide Urotensin-II Receptor Antagonists: A New Ligand Class Based on Piperazino-Phthalimide and Piperazino-Isoindolinone Subunits

Edward C. Lawson, Diane K. Luci, Shyamali Ghosh, William A. Kinney, Charles H. Reynolds, Jenson Qi, Charles E. Smith, Yuanping Wang, Lisa K. Minor, Barbara J. Haertlein, Tom J. Parry, Bruce P. Damiano and Bruce E. Maryanoff
Publication Date (Web): September 4, 2009 (Article)
DOI: 10.1021/jm900683d

September 1, 2009

A Strategy to Minimize Reactive Metabolite Formation: Discovery of (S)-4-(1-Cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a Potent, Orally Bioavailable Corticotropin-Releasing Factor-1 Receptor Antagonist

Richard A. Hartz, Vijay T. Ahuja, Xiaoliang Zhuo, Ronald J. Mattson, Derek J. Denhart, Jeffrey A. Deskus, Vivekananda M. Vrudhula, Senliang Pan, Jonathan L. Ditta, Yue-Zhong Shu, James E. Grace, Kimberley A. Lentz, Snjezana Lelas, Yu-Wen Li, Thaddeus F. Molski, Subramaniam Krishnananthan, Henry Wong, Jingfang Qian-Cutrone, Richard Schartman, Rex Denton, Nicholas J. Lodge, Robert Zaczek, John E. Macor and Joanne J. Bronson
Publication Date (Web): September 1, 2009 (Article)
DOI: 10.1021/jm900716v

September 3, 2009

(3R,5S,7as)-(3,5-Bis(4-fluorophenyl)tetrahydro-1H-oxazolo[3,4-c]oxazol-7a-yl)methanol, a Novel Neuroprotective Agent

Kelly E. Desino, Sabah Ansar, Gunda I. Georg, Richard H. Himes, Mary Lou Michaelis, Douglas R. Powell, Emily A. Reiff, Hanumaiah Telikepalli and Kenneth L. Audus
Publication Date (Web): September 3, 2009 (Article)
DOI: 10.1021/jm900254k

August 25, 2009

Synthesis and Characterization of Environment-Sensitive Fluorescent Ligands for Human 5-HT1A Receptors with 1-Arylpiperazine Structure

Enza Lacivita, Marcello Leopoldo, Anna Carmela Masotti, Carmela Inglese, Francesco Berardi, Roberto Perrone, Sourav Ganguly, Md Jafurulla and Amitabha Chattopadhyay
Publication Date (Web): August 25, 2009 (Brief Article)
DOI: 10.1021/jm900706d

Discovery of Potent and Selective Histone Deacetylase Inhibitors via Focused Combinatorial Libraries of Cyclic α3β-Tetrapeptides

Christian A. Olsen and M. Reza Ghadiri
Publication Date (Web): August 25, 2009 (Article)
DOI: 10.1021/jm900850t

August 26, 2009

Synthesis and In Vitro Opioid Receptor Functional Antagonism of Methyl-Substituted Analogues of (3R)-7-Hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic)

Juan Pablo Cueva, Tingwei Bill Cai, S. Wayne Mascarella, James B. Thomas, Hernn A. Navarro and F. Ivy Carroll
Publication Date (Web): August 26, 2009 (Article)
DOI: 10.1021/jm900756t

August 24, 2009

Eleven Amino Acid Glucagon-like Peptide-1 Receptor Agonists with Antidiabetic Activity

Claudio Mapelli, Sesha I. Natarajan, Jean-Philippe Meyer, Margarita M. Bastos, Michael S. Bernatowicz, Ving G. Lee, Jelka Pluscec, Douglas J. Riexinger, Ellen S. Sieber-McMaster, Keith L. Constantine, Constance A. Smith-Monroy, Rajasree Golla, Zhengping Ma, Daniel A. Longhi, Dan Shi, Li Xin, Joseph R. Taylor, Barry Koplowitz, Cecilia L. Chi, Ashish Khanna, Gordon W. Robinson, Ramakrishna Seethala, Ildiko A. Antal-Zimanyi, Robert H. Stoffel, Songping Han, Jean M. Whaley, Christine S. Huang, John Krupinski and William R. Ewing
Publication Date (Web): August 24, 2009 (Article)
DOI: 10.1021/jm900752a

August 19, 2009

Pyrrolidine Analogues of Lobelane: Relationship of Affinity for the Dihydrotetrabenazine Binding Site with Function of the Vesicular Monoamine Transporter 2 (VMAT2)

Ashish P. Vartak, Justin R. Nickell, Jaturaporn Chagkutip, Linda P. Dwoskin and Peter A. Crooks
Publication Date (Web): August 19, 2009 (Brief Article)
DOI: 10.1021/jm900770h

August 12, 2009

Design, Synthesis, and Examination of Neuron Protective Properties of Alkenylated and Amidated Dehydro-Silybin Derivatives

Lei Xiang Yang, Ke Xin Huang, Hai Bo Li, Jing Xu Gong, Feng Wang, Yu Bing Feng, Qiao Feng Tao, Yi Hang Wu, Xiao Kun Li, Xiu Mei Wu, Su Zeng, Shawn Spencer, Yu Zhao and Jia Qu
Publication Date (Web): August 12, 2009 (Article)
DOI: 10.1021/jm900735p

August 10, 2009

Vascular Disrupting Activity of Tubulin-Binding 1,5-Diaryl-1H-imidazoles

Katiuscia Bonezzi, Giulia Taraboletti, Patrizia Borsotti, Fabio Bellina, Renzo Rossi and Raffaella Giavazzi
Publication Date (Web): August 10, 2009 (Brief Article)
DOI: 10.1021/jm900968s

August 5, 2009

Discovery of Trp-His and His-Arg Analogues as New Structural Classes of Short Antimicrobial Peptides

Rohit K. Sharma, Ravi P. Reddy, Werner Tegge and Rahul Jain
Publication Date (Web): August 5, 2009 (Article)
DOI: 10.1021/jm900622d

August 3, 2009

Synthesis of New Linear Guanidines and Macrocyclic Amidinourea Derivatives Endowed with High Antifungal Activity against Candida spp. and Aspergillus spp.

Fabrizio Manetti, Daniele Castagnolo, Francesco Raffi, Alessandra T. Zizzari, Suvi Rajamki, Silvia D’Arezzo, Paolo Visca, Alessandra Cona, Maria Enrica Fracasso, Denise Doria, Brunella Posteraro, Maurizio Sanguinetti, Giovanni Fadda and Maurizio Botta
Publication Date (Web): August 3, 2009 (Letter)
DOI: 10.1021/jm900760k

July 31, 2009

Synthesis and Biological Evaluation of C-5 Methyl Substituted 4-Arylthio and 4-Aryloxy-3-Iodopyridin-2(1H)-one Type Anti-HIV Agents

Jrme Guillemont, Abdellah Benjahad, Said Oumouch, Laurence Decrane, Patrice Palandjian, Daniel Vernier, Laurence Queguiner, Koen Andries, Marie-Pierre de Bthune, Kurt Hertogs, David S. Grierson and Chi Hung Nguyen
Publication Date (Web): July 31, 2009 (Article)
DOI: 10.1021/jm900802y

July 30, 2009

Crystallographic Snapshots of Nonaged and Aged Conjugates of Soman with Acetylcholinesterase, and of a Ternary Complex of the Aged Conjugate with Pralidoxime

Benot Sanson, Florian Nachon, Jacques-Philippe Colletier, Marie-Thrse Froment, Lilly Toker, Harry M. Greenblatt, Joel L. Sussman, Yaacov Ashani, Patrick Masson, Israel Silman and Martin Weik
Publication Date (Web): July 30, 2009 (Article)
DOI: 10.1021/jm900433t

July 27, 2009

Preclinical Efficacy of a Carboxylesterase 2-Activated Prodrug of Doxazolidine

Benjamin L. Barthel, Zhiyong Zhang, Daniel L. Rudnicki, Christopher D. Coldren, Margaret Polinkovsky, Hengrui Sun, Gary G. Koch, Daniel C. F. Chan and Tad H. Koch
Publication Date (Web): July 27, 2009 (Article)
DOI: 10.1021/jm900694z

Univalent and Bivalent Ligands of Butorphan: Characteristics of the Linking Chain Determine the Affinity and Potency of Such Opioid Ligands

Michael Decker, Brian S. Fulton, Bin Zhang, Brian I. Knapp, Jean M. Bidlack and John L. Neumeyer
Publication Date (Web): July 27, 2009 (Article)
DOI: 10.1021/jm900379p

July 24, 2009

Probes for Narcotic Receptor Mediated Phenomena. 39. Enantiomeric N-Substituted Benzofuro[2,3-c]pyridin-6-ols: Synthesis and Topological Relationship to Oxide-Bridged Phenylmorphans

Yi Zhang, Yong Sok Lee, Richard B. Rothman, Christina M. Dersch, Jeffrey R. Deschamps, Arthur E. Jacobson and Kenner C. Rice
Publication Date (Web): July 24, 2009 (Article)
DOI: 10.1021/jm9004225

July 21, 2009

Discovery of Dermorphin-Based Affinity Labels with Subnanomolar Affinity for Mu Opioid Receptors

Bhaswati Sinha, Zhengyu Cao, Thomas F. Murray and Jane V. Aldrich
Publication Date (Web): July 21, 2009 (Letter)
DOI: 10.1021/jm9007592

High Lipophilicity of meta Mn(III) N-Alkylpyridylporphyrin-Based Superoxide Dismutase Mimics Compensates for Their Lower Antioxidant Potency and Makes Them as Effective as Ortho Analogues in Protecting Superoxide Dismutase-Deficient Escherichia coli

Ivan Kos, Ludmil Benov, Ivan Spasojevi, Jlio S. Rebouas and Ines Batini-Haberle
Publication Date (Web): July 21, 2009 (Brief Article)
DOI: 10.1021/jm900576g

July 17, 2009

Increasing Selectivity of CC Chemokine Receptor 8 Antagonists by Engineering Nondesolvation Related Interactions with the Intended and Off-Target Binding Sites

Igor Shamovsky, Chris de Graaf, Lisa Alderin, Malena Bengtsson, Hkan Bladh, Lena Brjesson, Stephen Connolly, Hazel J. Dyke, Marco van den Heuvel, Henrik Johansson, Bo-Gran Josefsson, Anna Kristoffersson, Tero Linnanen, Annea Lisius, Roope Mnnikk, Bo Nordn, Steve Price, Lena Ripa, Didier Rognan, Alexander Rosendahl, Marco Skrinjar and Klaus Urbahns
Publication Date (Web): July 17, 2009 (Article)
DOI: 10.1021/jm900713y

Small-Sized Human Immunodeficiency Virus Type-1 Protease Inhibitors Containing Allophenylnorstatine to Explore the S2′ Pocket

Koushi Hidaka, Tooru Kimura, Hamdy M. Abdel-Rahman, Jeffrey-Tri Nguyen, Keith F. McDaniel, William E. Kohlbrenner, Akhteruzzaman Molla, Motoyasu Adachi, Taro Tamada, Ryota Kuroki, Noriko Katsuki, Yoshiaki Tanaka, Hikaru Matsumoto, Jun Wang, Yoshio Hayashi, Dale J. Kempf and Yoshiaki Kiso
Publication Date (Web): July 17, 2009 (Article)
DOI: 10.1021/jm9005115

July 14, 2009

New Arylthioindoles and Related Bioisosteres at the Sulfur Bridging Group. 4. Synthesis, Tubulin Polymerization, Cell Growth Inhibition, and Molecular Modeling Studies

Giuseppe La Regina, Taradas Sarkar, Ruoli Bai, Michael C. Edler, Roberto Saletti, Antonio Coluccia, Francesco Piscitelli, Lara Minelli, Valerio Gatti, Carmela Mazzoccoli, Vanessa Palermo, Cristina Mazzoni, Claudio Falcone, Anna Ivana Scovassi, Vincenzo Giansanti, Pietro Campiglia, Amalia Porta, Bruno Maresca, Ernest Hamel, Andrea Brancale, Ettore Novellino and Romano Silvestri
Publication Date (Web): July 14, 2009 (Article)
DOI: 10.1021/jm900016t

July 16, 2009

Neglected Tropical Diseases: Multi-Target-Directed Ligands in the Search for Novel Lead Candidates against Trypanosoma and Leishmania

Andrea Cavalli and Maria Laura Bolognesi
Publication Date (Web): July 16, 2009 (Perspective)
DOI: 10.1021/jm9004835

July 8, 2009

Malaria-Infected Mice Live until at Least Day 30 after a New Monomeric Trioxane Combined with Mefloquine Are Administered Together in a Single Low Oral Dose

Lauren E. Woodard, Wonsuk Chang, Xiaochun Chen, Jun O. Liu, Theresa A. Shapiro and Gary H. Posner
Publication Date (Web): July 8, 2009 (Article)
DOI: 10.1021/jm9005934

July 10, 2009

3,4-Diaryl-isoxazoles and -imidazoles as Potent Dual Inhibitors of p38α Mitogen Activated Protein Kinase and Casein Kinase 1δ

Christian Peifer, Mohammed Abadleh, Joachim Bischof, Dominik Hauser, Verena Schattel, Heidrun Hirner, Uwe Knippschild and Stefan Laufer
Publication Date (Web): July 10, 2009 (Article)
DOI: 10.1021/jm9005127

July 7, 2009

Synthesis and in Vitro Evaluation of N-Substituted Maleimide Derivatives as Selective Monoglyceride Lipase Inhibitors

Nicolas Matuszak, Giulio G. Muccioli, Geoffray Labar and Didier M. Lambert
Publication Date (Web): July 7, 2009 (Article)
DOI: 10.1021/jm900461w

July 6, 2009

Nucleoside-5′-monophosphates as Prodrugs of Adenosine A2A Receptor Agonists Activated by ecto-5′-Nucleotidase†

Contribution to celebrate the 100th anniversary of the Division of Medicinal Chemistry of the American Chemical Society.

Ali El-Tayeb, Jamshed Iqbal, Andrea Behrenswerth, Michael Romio, Marion Schneider, Herbert Zimmermann, Jrgen Schrader and Christa E. Mller
Publication Date (Web): July 6, 2009 (Article)
DOI: 10.1021/jm900538v

July 2, 2009

Modifications at the C-Terminus To Improve Pyrrole−Imidazole Polyamide Activity in Cell Culture

Claire S. Jacobs and Peter B. Dervan
Publication Date (Web): July 2, 2009 (Article)
DOI: 10.1021/jm900256f

June 18, 2009

Discovery of the First Series of Small Molecule H5N1 Entry Inhibitors

Gaopeng Song, Sen Yang, Wei Zhang, Yingli Cao, Peng Wang, Ning Ding, Zaihong Zhang, Ying Guo and Yingxia Li
Publication Date (Web): June 18, 2009 (Letter)
DOI: 10.1021/jm900275m

June 9, 2009

Discovery of Potent Competitive Inhibitors of Indoleamine 2,3-Dioxygenase with in Vivo Pharmacodynamic Activity and Efficacy in a Mouse Melanoma Model

Eddy W. Yue, Brent Douty, Brian Wayland, Michael Bower, Xiangdong Liu, Lynn Leffet, Qian Wang, Kevin J. Bowman, Michael J. Hansbury, Changnian Liu, Min Wei, Yanlong Li, Richard Wynn, Timothy C. Burn, Holly K. Koblish, Jordan S. Fridman, Brian Metcalf, Peggy A. Scherle and Andrew P. Combs
Publication Date (Web): June 9, 2009 (Letter)
DOI: 10.1021/jm900518f

June 15, 2009

Betulinic Acid Derivatives as Human Immunodeficiency Virus Type 2 (HIV-2) Inhibitors

Zhao Dang, Weihong Lai, Keduo Qian, Phong Ho, Kuo-Hsiung Lee, Chin-Ho Chen and Li Huang
Publication Date (Web): June 15, 2009 (Brief Article)
DOI: 10.1021/jm9004253

June 8, 2009

Functionalized Congeners of A3 Adenosine Receptor-Selective Nucleosides Containing a Bicyclo[3.1.0]hexane Ring System

Dilip K. Tosh, Moshe Chinn, Andrei A. Ivanov, Athena M. Klutz, Zhan-Guo Gao and Kenneth A. Jacobson
Publication Date (Web): June 8, 2009 (Article)
DOI: 10.1021/jm900426g

April 23, 2009

Novel, Broad-Spectrum Anticonvulsants Containing a Sulfamide Group: Advancement of N-((Benzo[b]thien-3-yl)methyl)sulfamide (JNJ-26990990) into Human Clinical Studies

Michael H. Parker, Virginia L. Smith-Swintosky, David F. McComsey, Yifang Huang, Douglas Brenneman, Brian Klein, Ewa Malatynska, H. Steve White, Michael E. Milewski, Mark Herb, Michael F. A. Finley, Yi Liu, Mary Lou Lubin, Ning Qin, Robert Iannucci, Laurent Leclercq, Filip Cuyckens, Allen B. Reitz and Bruce E. Maryanoff
Publication Date (Web): April 23, 2009 (Article)
DOI: 10.1021/jm801432r

April 14, 2009

Identification and Structure−Activity Relationships of Chromene-Derived Selective Estrogen Receptor Modulators for Treatment of Postmenopausal Symptoms

Nareshkumar Jain, Jiayi Xu, Ramesh M. Kanojia, Fuyong Du, Guo Jian-Zhong, Emmanuel Pacia, Muh-Tsann Lai, Amy Musto, George Allan, Michael Reuman, Xun Li, DoWon Hahn, Martin Cousineau, Sean Peng, David Ritchie, Ronald Russell, Scott Lundeen and Zhihua Sui
Publication Date (Web): April 14, 2009 (Article)
DOI: 10.1021/jm900146e

October 23, 2009

Identification of Lead Compounds As Antagonists of Protein Bcl-xL with a Diversity-Oriented Multidisciplinary Approach

Simone Di Micco, Romina Vitale, Maurizio Pellecchia, Michele F. Rega, Renata Riva, Andrea Basso and Giuseppe Bifulco
Publication Date (Web): October 23, 2009 (Article)
DOI: 10.1021/jm9010687

October 22, 2009

Aza-Peptidyl Michael Acceptor and Epoxide Inhibitors—Potent and Selective Inhibitors of Schistosoma mansoni and Ixodes ricinus Legumains (Asparaginyl Endopeptidases)

Asli Ovat, Fanuel Muindi, Crystal Fagan, Michelle Brouner, Elizabeth Hansell, Jan Dvok, Daniel Sojka, Petr Kopek, James H. McKerrow, Conor R. Caffrey and James C. Powers
Publication Date (Web): October 22, 2009 (Article)
DOI: 10.1021/jm900849h
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