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    • J. Med. Chem.
    • ACS Med. Chem. Lett.

ACS Medicinal Chemistry Letters is now the exclusive source for all Letters in medicinal chemistry. The Journal of Medicinal Chemistry continues to publish Articles, Brief Articles, and Perspectives. View the first articles from ACS Medicinal Chemistry Letters, free for a limited time.

Articles ASAP (As Soon As Publishable)

ASAP articles are edited and published online ahead of print.

ACS AuthorChoice indicates the article is freely available through sponsorship by the author or related funding agency. More about this program.
For Selected Content:

February 9, 2010

Biological and Biophysical Properties of the Histone Deacetylase Inhibitor Suberoylanilide Hydroxamic Acid Are Affected by the Presence of Short Alkyl Groups on the Phenyl Ring

Frdrik Oger, Aurlien Lecorgne, Elisa Sala, Vanessa Nardese, Florence Demay, Soizic Chevance, Danielle C. Desravines, Nataliia Aleksandrova, Rmy Le Guvel, Simone Lorenzi, Andrea R. Beccari, Peter Barath, Darren J. Hart, Arnaud Bondon, Daniele Carettoni, Grard Simonneaux and Gilles Salbert
Publication Date (Web): February 9, 2010 (Article)
DOI: 10.1021/jm901561u
Abstract | Supporting Info
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Synthesis and Evaluation of Paracetamol Esters As Novel Fatty Acid Amide Hydrolase Inhibitors

Valentina Onnis, Cenzo Congiu, Emmelie Bjrklund, Franziska Hempel, Emma Sderstrm and Christopher J. Fowler
Publication Date (Web): February 9, 2010 (Article)
DOI: 10.1021/jm901891p
Abstract | Supporting Info
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Discovery of 7-(4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDC-101) as a Potent Multi-Acting HDAC, EGFR, and HER2 Inhibitor for the Treatment of Cancer

Xiong Cai, Hai-Xiao Zhai, Jing Wang, Jeffrey Forrester, Hui Qu, Ling Yin, Cheng-Jung Lai, Rudi Bao and Changgeng Qian
Publication Date (Web): February 9, 2010 (Article)
DOI: 10.1021/jm901453q
Abstract | Supporting Info
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Discovery of 1-[3-(4-Bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (Nelotanserin) and Related 5-Hydroxytryptamine2A Inverse Agonists for the Treatment of Insomnia

Bradley R. Teegarden, Hongmei Li, Honnappa Jayakumar, Sonja Strah-Pleynet, Peter I. Dosa, Susan D. Selaya, Naomi Kato, Katie H. Elwell, Jarrod Davidson, Karen Cheng, Hazel Saldana, John M. Frazer, Kevin Whelan, Jonathan Foster, Stephan Espitia, Robert R. Webb, Nigel R. A. Beeley, William Thomsen, Stephen R. Morairty, Thomas S. Kilduff and Hussien A. Al-Shamma
Publication Date (Web): February 9, 2010 (Article)
DOI: 10.1021/jm9007328
Abstract
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February 8, 2010

Identification of Potent Pyrazolo[4,3-h]quinazoline-3-carboxamides as Multi-Cyclin-Dependent Kinase Inhibitors

Gabriella Traquandi, Marina Ciomei, Dario Ballinari, Elena Casale, Nicoletta Colombo, Valter Croci, Francesco Fiorentini, Antonella Isacchi, Antonio Longo, Ciro Mercurio, Achille Panzeri, Wilma Pastori, Paolo Pevarello, Daniele Volpi, Patrick Roussel, Anna Vulpetti and Maria Gabriella Brasca
Publication Date (Web): February 8, 2010 (Article)
DOI: 10.1021/jm901710h
Abstract | Supporting Info
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Piperazinyl Glutamate Pyridines as Potent Orally Bioavailable P2Y12 Antagonists for Inhibition of Platelet Aggregation

John J. Parlow, Mary W. Burney, Brenda L. Case, Thomas J. Girard, Kerri A. Hall, Peter K. Harris, Ronald R. Hiebsch, Rita M. Huff, Rhonda M. Lachance, Deborah A. Mischke, Stephen R. Rapp, Rhonda S. Woerndle and Michael D. Ennis
Publication Date (Web): February 8, 2010 (Article)
DOI: 10.1021/jm901518t
Abstract | Supporting Info
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February 4, 2010

Incorporation of Fluorinated Phenylalanine Generates Highly Specific Inhibitor of Proteasome’s Chymotrypsin-like Sites

Paul P. Geurink, Nora Liu, Michiel P. Spaans, Sondra L. Downey, Adrianus M. C. H. van den Nieuwendijk, Gijsbert A. van der Marel, Alexei F. Kisselev, Bogdan I. Florea and Herman S. Overkleeft
Publication Date (Web): February 4, 2010 (Brief Article)
DOI: 10.1021/jm9015685
Abstract | Supporting Info
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Michael Acceptor Based Antiplasmodial and Antitrypanosomal Cysteine Protease Inhibitors with Unusual Amino Acids

Alexander Breuning, Bjrn Degel, Franziska Schulz, Christian Bchold, Martin Stempka, Uwe Machon, Saskia Heppner, Christoph Gelhaus, Matthias Leippe, Matthias Leyh, Caroline Kisker, Jennifer Rath, August Stich, Jiri Gut, Philip J. Rosenthal, Carsten Schmuck and Tanja Schirmeister
Publication Date (Web): February 4, 2010 (Article)
DOI: 10.1021/jm900946n
Abstract | Supporting Info
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New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays

Jonathan B. Baell and Georgina A. Holloway
Publication Date (Web): February 4, 2010 (Article)
DOI: 10.1021/jm901137j
Abstract | Supporting Info
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Photooxidation and Phototoxicity of π-Extended Squaraines

Valentina Rapozzi, Luca Beverina, Patrizio Salice, Giorgio A. Pagani, Monica Camerin and Luigi E. Xodo
Publication Date (Web): February 4, 2010 (Article)
DOI: 10.1021/jm901727j
Abstract | Supporting Info
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February 3, 2010

New Benzophenone-Derived Bisphosphonium Salts as Leishmanicidal Leads Targeting Mitochondria through Inhibition of Respiratory Complex II

J. Romn Luque-Ortega, Peter Reuther, Luis Rivas and Christophe Dardonville
Publication Date (Web): February 3, 2010 (Article)
DOI: 10.1021/jm901677h
Abstract
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Structure of Human G Protein-Coupled Receptor Kinase 2 in Complex with the Kinase Inhibitor Balanol

John J. G. Tesmer, Valerie M. Tesmer, David T. Lodowski, Henning Steinhagen and Jochen Huber
Publication Date (Web): February 3, 2010 (Brief Article)
DOI: 10.1021/jm9017515
Abstract | Supporting Info
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Synthesis and Biological Evaluation of Polysulfated Oligosaccharide Glycosides as Inhibitors of Angiogenesis and Tumor Growth

Ken D. Johnstone, Tomislav Karoli, Ligong Liu, Keith Dredge, Elizabeth Copeman, Cai Ping Li, Kat Davis, Edward Hammond, Ian Bytheway, Edmund Kostewicz, Francis C. K. Chiu, David M. Shackleford, Susan A. Charman, William N. Charman, Job Harenberg, Thomas J. Gonda and Vito Ferro
Publication Date (Web): February 3, 2010 (Article)
DOI: 10.1021/jm901449m
Abstract | Supporting Info
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Design and Synthesis of Potent and Selective BACE-1 Inhibitors

Catarina Bjrklund, Stefan Oscarson, Kurt Benkestock, Neera Borkakoti, Katarina Jansson, Jimmy Lindberg, Lotta Vrang, Anders Hallberg, Åsa Rosenquist and Bertil Samuelsson
Publication Date (Web): February 3, 2010 (Article)
DOI: 10.1021/jm901168f
Abstract | Supporting Info
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Identification and Characterization of 4-Chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a Selective and Irreversible Peroxisome Proliferator-Activated Receptor δ (PPARδ) Antagonist

Barry G. Shearer, Robert W. Wiethe, Adam Ashe, Andrew N. Billin, James M. Way, Thomas B. Stanley, Craig D. Wagner, Robert X. Xu, Lisa M. Leesnitzer, Raymond V. Merrihew, Todd W. Shearer, Michael R. Jeune, John C. Ulrich and Timothy M. Willson
Publication Date (Web): February 3, 2010 (Brief Article)
DOI: 10.1021/jm900464j
Abstract
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February 2, 2010

Structure Based Drug Design: Development of Potent and Selective Factor IXa (FIXa) Inhibitors

Shouming Wang, Richard Beck, Andrew Burd, Toby Blench, Frederic Marlin, Tenagne Ayele, Stuart Buxton, Claudio Dagostin, Maja Malic, Rina Joshi, John Barry, Mohammed Sajad, Chiming Cheung, Shaheda Shaikh, Suresh Chahwala, Chaman Chander, Christine Baumgartner, Hans-Peter Holthoff, Elizabeth Murray, Michael Blackney and Amanda Giddings
Publication Date (Web): February 2, 2010 (Article)
DOI: 10.1021/jm901476x
Abstract | Supporting Info
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1-(Indolin-1-yl)-1-phenyl-3-propan-2-olamines as Potent and Selective Norepinephrine Reuptake Inhibitors

An T. Vu, Stephen T. Cohn, Puwen Zhang, Callain Y. Kim, Paige E. Mahaney, Jenifer A. Bray, Grace H. Johnston, Elizabeth J. Koury, Scott A. Cosmi, Darlene C. Deecher, Valerie A. Smith, James E. Harrison, Liza Leventhal, Garth T. Whiteside, Jeffrey D. Kennedy and Eugene J. Trybulski
Publication Date (Web): February 2, 2010 (Article)
DOI: 10.1021/jm901559e
Abstract
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Studies of Benzothiophene Template as Potent Factor IXa (FIXa) Inhibitors in Thrombosis

Shouming Wang, Richard Beck, Toby Blench, Andrew Burd, Stuart Buxton, Maja Malic, Tenagne Ayele, Shaheda Shaikh, Suresh Chahwala, Chaman Chander, Richard Holland, Sandrine Merette, Lihua Zhao, Michael Blackney and Alexandra Watts
Publication Date (Web): February 2, 2010 (Article)
DOI: 10.1021/jm901475e
Abstract | Supporting Info
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Discovery of Novel Fibroblast Growth Factor Receptor 1 Kinase Inhibitors by Structure-Based Virtual Screening

Krishna P. Ravindranathan, Valsan Mandiyan, Anil R. Ekkati, Jae H. Bae, Joseph Schlessinger and William L. Jorgensen
Publication Date (Web): February 2, 2010 (Article)
DOI: 10.1021/jm901386e
Abstract | Supporting Info
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February 1, 2010

Engineering Galanin Analogues That Discriminate between GalR1 and GalR2 Receptor Subtypes and Exhibit Anticonvulsant Activity following Systemic Delivery

Charles R. Robertson, Erika Adkins Scholl, Timothy H. Pruess, Brad R. Green, H. Steve White and Grzegorz Bulaj
Publication Date (Web): February 1, 2010 (Brief Article)
DOI: 10.1021/jm9018349
Abstract | Supporting Info
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Insight into Binding of Phosphodiesterase-9A Selective Inhibitors by Crystal Structures and Mutagenesis

Huanchen Wang, Xuan Luo, Mengchun Ye, Jing Hou, Howard Robinson and Hengming Ke
Publication Date (Web): February 1, 2010 (Article)
DOI: 10.1021/jm901519f
Abstract
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Synthesis, Biological Evaluation, and Molecular Modeling of 1-Benzyl-1H-imidazoles as Selective Inhibitors of Aldosterone Synthase (CYP11B2)

Luc Roumen, Joris W. Peeters, Judith M. A. Emmen, Ilona P. E. Beugels, Erica M. G. Custers, Marcel de Gooyer, Ralf Plate, Koen Pieterse, Peter A. J. Hilbers, Jos F. M. Smits, Jef A. J. Vekemans, Dirk Leysen, Harry C. J. Ottenheijm, Henk M. Janssen and J. J. Rob Hermans
Publication Date (Web): February 1, 2010 (Article)
DOI: 10.1021/jm901356d
Abstract | Supporting Info
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New Structures and Bioactivity Properties of Jasplakinolide (Jaspamide) Analogues from Marine Sponges

Sarah J. Robinson, Brandon I. Morinaka, Taro Amagata, Karen Tenney, Walter M. Bray, Nadine C. Gassner, R. Scott Lokey and Phillip Crews
Publication Date (Web): February 1, 2010 (Article)
DOI: 10.1021/jm9013554
Abstract | Supporting Info
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Evolving Carbapenemases: Can Medicinal Chemists Advance One Step Ahead of the Coming Storm?

Peter Oelschlaeger, Ni Ai, Kevin T. DuPrez, William J. Welsh and Jeffrey H. Toney
Publication Date (Web): February 1, 2010 (Perspective)
DOI: 10.1021/jm9012938
Abstract | Supporting Info
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January 29, 2010

A Novel Cationic Lipophosphoramide with Diunsaturated Lipid Chains: Synthesis, Physicochemical Properties, and Transfection Activities

Tony Le Gall, Damien Loizeau, Erwan Picquet, Nathalie Carmoy, Jean-Jacques Yaouanc, Laure Burel-Deschamps, Pascal Delpine, Philippe Giamarchi, Paul-Alain Jaffrs, Pierre Lehn and Tristan Montier
Publication Date (Web): January 29, 2010 (Article)
DOI: 10.1021/jm900897a
Abstract | Supporting Info
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5-Modified-2′-dU and 2′-dC as Mutagenic Anti HIV-1 Proliferation Agents: Synthesis and Activity

Yazan El Safadi, Jean-Christophe Paillart, Graldine Laumond, Anne-Marie Aubertin, Alain Burger, Roland Marquet and Valrie Vivet-Boudou
Publication Date (Web): January 29, 2010 (Article)
DOI: 10.1021/jm901758f
Abstract | Supporting Info
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Studies of the Synthesis of All Stereoisomers of MG-132 Proteasome Inhibitors in the Tumor Targeting Approach

Michał Mroczkiewicz, Katarzyna Winkler, Dominika Nowis, Grzegorz Placha, Jakub Golab and Ryszard Ostaszewski
Publication Date (Web): January 29, 2010 (Article)
DOI: 10.1021/jm901619n
Abstract | Supporting Info
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January 28, 2010

Synthesis of New Thienyl Ring Containing HIV-1 Protease Inhibitors: Promising Preliminary Pharmacological Evaluation against Recombinant HIV-1 Proteases

Carlo Bonini, Lucia Chiummiento, Margherita De Bonis, Nadia Di Blasio, Maria Funicello, Paolo Lupattelli, Rocco Pandolfo, Francesco Tramutola and Federico Berti
Publication Date (Web): January 28, 2010 (Article)
DOI: 10.1021/jm900846f
Abstract | Supporting Info
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New Fluorinated 1,2,4-Benzothiadiazine 1,1-Dioxides: Discovery of an Orally Active Cognitive Enhancer Acting through Potentiation of the 2-Amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic Acid Receptors

Pierre Francotte, Eric Goffin, Pierre Fraikin, Pierre Lestage, Jean-Claude Van Heugen, Florian Gillotin, Laurence Danober, Jean-Yves Thomas, Patrice Chiap, Daniel-Henri Caignard, Bernard Pirotte and Pascal de Tullio
Publication Date (Web): January 28, 2010 (Article)
DOI: 10.1021/jm901495t
Abstract | Supporting Info
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Antisense Oligonucleotides Containing Conformationally Constrained 2′,4′-(N-Methoxy)aminomethylene and 2′,4′-Aminooxymethylene and 2′-O,4′-C-Aminomethylene Bridged Nucleoside Analogues Show Improved Potency in Animal Models

Thazha P. Prakash, Andrew Siwkowski, Charles R. Allerson, Michael T. Migawa, Sam Lee, Hans J. Gaus, Chris Black, Punit P. Seth, Eric E. Swayze and Balkrishen Bhat
Publication Date (Web): January 28, 2010 (Article)
DOI: 10.1021/jm9013295
Abstract | Supporting Info
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Novel Inhibitors of Dengue Virus Methyltransferase: Discovery by in Vitro-Driven Virtual Screening on a Desktop Computer Grid

Michael Podvinec, Siew Pheng Lim, Tobias Schmidt, Marco Scarsi, Daying Wen, Louis-Sebastian Sonntag, Paul Sanschagrin, Peter S. Shenkin and Torsten Schwede
Publication Date (Web): January 28, 2010 (Article)
DOI: 10.1021/jm900776m
Abstract | Supporting Info
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Nitric Oxide Donors or Nitrite Counteract Copper-[dithiocarbamate]2-Mediated Tumor Cell Death and Inducible Nitric Oxide Synthase Down-Regulation: Possible Role of a Nitrosyl-Copper [Dithiocarbamate]2 Complex

Maricela Viola Rhenals, Mary Strasberg-Rieber and Manuel Rieber
Publication Date (Web): January 28, 2010 (Article)
DOI: 10.1021/jm901314r
Abstract
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January 27, 2010

Structure−Activity Relationships Studies in a Series of N,N-Bis(alkanol)amine Aryl Esters as P-Glycoprotein (Pgp) Dependent Multidrug Resistance (MDR) Inhibitors

Cecilia Martelli, Marcella Coronnello, Silvia Dei, Dina Manetti, Francesca Orlandi, Serena Scapecchi, Maria Novella Romanelli, Milena Salerno, Enrico Mini and Elisabetta Teodori
Publication Date (Web): January 27, 2010 (Article)
DOI: 10.1021/jm9016174
Abstract | Supporting Info
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Subtlety of the Structure−Affinity and Structure−Efficacy Relationships around a Nonpeptide Oxytocin Receptor Agonist

Marie-Cline Frantz, Jordi Rodrigo, Laure Boudier, Thierry Durroux, Bernard Mouillac and Marcel Hibert
Publication Date (Web): January 27, 2010 (Article)
DOI: 10.1021/jm901084f
Abstract | Supporting Info
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January 26, 2010

Two-Step Synthesis of Galactosylated Human Serum Albumin as a Targeted Optical Imaging Agent for Peritoneal Carcinomatosis

Celeste Aida S. Regino, Mikako Ogawa, Raphael Alford, Karen J. Wong, Noboyuki Kosaka, Mark Williams, Brian J. Feild, Masatoshi Takahashi, Peter L. Choyke and Hisataka Kobayashi
Publication Date (Web): January 26, 2010 (Article)
DOI: 10.1021/jm901228u
Abstract | Supporting Info
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Synthesis and Preclinical Evaluations of 2-(2-Fluorophenyl)-6,7-methylenedioxyquinolin-4-one Monosodium Phosphate (CHM-1−P-Na) as a Potent Antitumor Agent

Li-Chen Chou, Chien-Ting Chen, Jang-Chang Lee, Tzong-Der Way, Chi-Hung Huang, Shih-Ming Huang, Che-Ming Teng, Takao Yamori, Tian-Shung Wu, Chung-Ming Sun, Du-Shieng Chien, Keduo Qian, Susan L. Morris-Natschke, Kuo-Hsiung Lee, Li-Jiau Huang and Sheng-Chu Kuo
Publication Date (Web): January 26, 2010 (Article)
DOI: 10.1021/jm901292j
Abstract | Supporting Info
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Current and Future Medical Approaches To Combat the Anthrax Threat

Dimitrios G. Bouzianas
Publication Date (Web): January 26, 2010 (Perspective)
DOI: 10.1021/jm901024b
Abstract
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Discovery and Clinical Evaluation of 1-{N-[2-(Amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a Thrombin Inhibitor with an Oxyguanidine P1 Motif

Tianbao Lu, Thomas Markotan, Shelley K. Ballentine, Edward C. Giardino, John Spurlino, Kathryn Brown, Bruce E. Maryanoff, Bruce E. Tomczuk, Bruce P. Damiano, Umesh Shukla, David End, Patricia Andrade-Gordon, Roger F. Bone and Mark R. Player
Publication Date (Web): January 26, 2010 (Article)
DOI: 10.1021/jm901802n
Abstract
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January 25, 2010

Characterization of Tunable Piperidine and Piperazine Carbamates as Inhibitors of Endocannabinoid Hydrolases

Jonathan Z. Long, Xin Jin, Alexander Adibekian, Weiwei Li and Benjamin F. Cravatt
Publication Date (Web): January 25, 2010 (Article)
DOI: 10.1021/jm9016976
Abstract
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Discovery and Optimization of Novel 3-Piperazinylcoumarin Antagonist of Chemokine-like Factor 1 with Oral Antiasthma Activity in Mice

Gang Li, Dongmei Wang, Mingna Sun, Guangyan Li, Jinfeng Hu, Yun Zhang, Yuhe Yuan, Haijie Ji, Naihong Chen and Gang Liu
Publication Date (Web): January 25, 2010 (Article)
DOI: 10.1021/jm901652p
Abstract | Supporting Info
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January 22, 2010

Exploring Epidermal Growth Factor Receptor (EGFR) Inhibitor Features: The Role of Fused Dioxygenated Rings on the Quinazoline Scaffold

Adriana Chilin, Maria Teresa Conconi, Giovanni Marzaro, Adriano Guiotto, Luca Urbani, Francesca Tonus and Pierpaolo Parnigotto
Publication Date (Web): January 22, 2010 (Brief Article)
DOI: 10.1021/jm901338g
Abstract | Supporting Info
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Structure-Based Discovery of Novel Chemotypes for Adenosine A2A Receptor Antagonists

Vsevolod Katritch, Veli-Pekka Jaakola, J. Robert Lane, Judy Lin, Adriaan P. IJzerman, Mark Yeager, Irina Kufareva, Raymond C. Stevens and Ruben Abagyan
Publication Date (Web): January 22, 2010 (Article)
DOI: 10.1021/jm901647p
Abstract | Supporting Info
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Improvement of Physiochemical Properties of the Tetrahydroazepinoindole Series of Farnesoid X Receptor (FXR) Agonists: Beneficial Modulation of Lipids in Primates

Joseph T. Lundquist, IV, Douglas C. Harnish, Callain Y. Kim, John F. Mehlmann, Rayomand J. Unwalla, Kristin M. Phipps, Matthew L. Crawley, Thomas Commons, Daniel M. Green, Weixin Xu, Wah-Tung Hum, Julius E. Eta, Irene Feingold, Vikram Patel, Mark J. Evans, KehDih Lai, Lisa Borges-Marcucci, Paige E. Mahaney and Jay E. Wrobel
Publication Date (Web): January 22, 2010 (Article)
DOI: 10.1021/jm901650u
Abstract
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Low Molecular Weight Antagonists of the Myelin-Associated Glycoprotein: Synthesis, Docking, and Biological Evaluation

Stefanie Mesch, Delia Moser, Daniel S. Strasser, Antje Kelm, Brian Cutting, Gianluca Rossato, Angelo Vedani, Hendrik Koliwer-Brandl, Matthias Wittwer, Said Rabbani, Oliver Schwardt, Soerge Kelm and Beat Ernst
Publication Date (Web): January 22, 2010 (Article)
DOI: 10.1021/jm901517k
Abstract | Supporting Info
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Corrections to Synthesis, Biological Evaluation, X-ray Structure, and Pharmacokinetics of Aminopyrimidine c-jun-N-terminal Kinase (JNK) Inhibitors

Ted Kamenecka, Rong Jiang, Xinyi Song, Derek Duckett, Weimin Chen, Yuan Yuan Ling, Jeff Habel, John D. Laughlin, Jeremy Chambers, Mariana Figuera-Losada, Michael D. Cameron, Li Lin, Claudia H. Ruiz and Philip V. LoGrasso
Publication Date (Web): January 22, 2010 (Addition/Correction)
DOI: 10.1021/jm1000425
Abstract
Original Article
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5-OMe-UDP is a Potent and Selective P2Y6-Receptor Agonist

Tamar Ginsburg-Shmuel, Michael Haas, Marlen Schumann, Georg Reiser, Ori Kalid, Noa Stern and Bilha Fischer
Publication Date (Web): January 22, 2010 (Article)
DOI: 10.1021/jm901450d
Abstract | Supporting Info
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January 21, 2010

Synthesis and Structure−Activity Relationships of Dimeric Peptide Antagonists of the Human Immunoglobulin G−Human Neonatal Fc Receptor (IgG−FcRn) Interaction

Kevin A. McDonnell, Susan C. Low, Todd Hoehn, Ryan Donnelly, Holly Palmieri, Cara Fraley, Paul Sakorafas and Adam R. Mezo
Publication Date (Web): January 21, 2010 (Article)
DOI: 10.1021/jm901128z
Abstract | Supporting Info
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Corrections to Aminoimidazoles as Potent and Selective Human β-Secretase (BACE1) Inhibitors

Michael S. Malamas, Jim Erdei, Iwan Gunawan, Keith Barnes, Matthew Johnson, Yu Hui, Jim Turner, Yun Hu, Erik Wagner, Kristi Fan, Andrea Olland, Jonathan Bard and Albert J. Robichaud
Publication Date (Web): January 21, 2010 (Addition/Correction)
DOI: 10.1021/jm901921x
Abstract
Original Article
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Single Agents with Designed Combination Chemotherapy Potential: Synthesis and Evaluation of Substituted Pyrimido[4,5-b]indoles as Receptor Tyrosine Kinase and Thymidylate Synthase Inhibitors and as Antitumor Agents

Aleem Gangjee, Nilesh Zaware, Sudhir Raghavan, Michael Ihnat, Satyendra Shenoy and Roy L. Kisliuk
Publication Date (Web): January 21, 2010 (Article)
DOI: 10.1021/jm9011142
Abstract | Supporting Info
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Anti-Influenza Drug Discovery: Structure−Activity Relationship and Mechanistic Insight into Novel Angelicin Derivatives

Jiann-Yih Yeh, Mohane Selvaraj Coumar, Jim-Tong Horng, Hui-Yi Shiao, Fu-Ming Kuo, Hui-Ling Lee, In-Chun Chen, Chun-Wei Chang, Wen-Fang Tang, Sung-Nain Tseng, Chi-Jene Chen, Shin-Ru Shih, John T.-A. Hsu, Chun-Chen Liao, Yu-Sheng Chao and Hsing-Pang Hsieh
Publication Date (Web): January 21, 2010 (Article)
DOI: 10.1021/jm901570x
Abstract | Supporting Info
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January 20, 2010

Nonpeptidic Tetrafluorophenoxymethyl Ketone Cruzain Inhibitors as Promising New Leads for Chagas Disease Chemotherapy

Katrien Brak, Iain D. Kerr, Kimberly T. Barrett, Nobuhiro Fuchi, Moumita Debnath, Kenny Ang, Juan C. Engel, James H. McKerrow, Patricia S. Doyle, Linda S. Brinen and Jonathan A. Ellman
Publication Date (Web): January 20, 2010 (Article)
DOI: 10.1021/jm901633v
Abstract | Supporting Info
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One Step Radiosynthesis of 6-[18F]Fluoronicotinic Acid 2,3,5,6-Tetrafluorophenyl Ester ([18F]F-Py-TFP): A New Prosthetic Group for Efficient Labeling of Biomolecules with Fluorine-18

Dag E. Olberg, Joseph M. Arukwe, David Grace, Ole K. Hjelstuen, Magne Solbakken, Grete M. Kindberg and Alan Cuthbertson
Publication Date (Web): January 20, 2010 (Article)
DOI: 10.1021/jm9015813
Abstract | Supporting Info
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Selective Inhibitors of the JMJD2 Histone Demethylases: Combined Nondenaturing Mass Spectrometric Screening and Crystallographic Approaches

Nathan R. Rose, Esther C. Y. Woon, Guy L. Kingham, Oliver N. F. King, Jasmin Mecinovi, Ian J. Clifton, Stanley S. Ng, Jobina Talib-Hardy, Udo Oppermann, Michael A. McDonough and Christopher J. Schofield
Publication Date (Web): January 20, 2010 (Article)
DOI: 10.1021/jm901680b
ACS AuthorChoice
Abstract | Supporting Info
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Natural Product Chemistry for Drug Discovery (RSC Biomolecular Sciences No. 18)

A. Douglas Kinghorn
Publication Date (Web): January 20, 2010 (Book Review)
DOI: 10.1021/jm100010y
Abstract
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De Novo Design of a Picomolar Nonbasic 5-HT1B Receptor Antagonist

David A. Nugiel, Jennifer R. Krumrine, Daniel C. Hill, James R. Damewood, Jr., Peter R. Bernstein, Cynthia D. Sobotka-Briner, JianWei Liu, Anna Zacco and M. Edward Pierson
Publication Date (Web): January 20, 2010 (Brief Article)
DOI: 10.1021/jm901200t
Abstract | Supporting Info
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Substituted Benzothiophene or Benzofuran Derivatives as a Novel Class of Bone Morphogenetic Protein-2 Up-Regulators: Synthesis, Structure−Activity Relationships, and Preventive Bone Loss Efficacies in Senescence Accelerated Mice (SAMP6) and Ovariectomized Rats

Hui-fang Guo, Hua-yi Shao, Zhao-yong Yang, Si-tu Xue, Xue Li, Zong-ying Liu, Xiao-bo He, Jian-dong Jiang, Yue-qin Zhang, Shu-yi Si and Zhuo-rong Li
Publication Date (Web): January 20, 2010 (Article)
DOI: 10.1021/jm901685n
Abstract | Supporting Info
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January 19, 2010

Book Review of Real World Drug Discovery. A Chemist’s Guide to Biotech and Pharmaceutical Research

Manfred E. Wolff
Publication Date (Web): January 19, 2010 (Book Review)
DOI: 10.1021/jm100011q
Abstract
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January 8, 2010

Inhibitors of Prolyl Oligopeptidases for the Therapy of Human Diseases: Defining Diseases and Inhibitors

Janice Lawandi, Sandrine Gerber-Lemaire, Lucienne Juillerat-Jeanneret and Nicolas Moitessier
Publication Date (Web): January 8, 2010 (Perspective)
DOI: 10.1021/jm901104g
Abstract
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January 4, 2010

Small Molecules and Stem Cells. Potency and Lineage Commitment: The New Quest for the Fountain of Youth

Agns I. Lukaszewicz, Michael K. McMillan and Michael Kahn
Publication Date (Web): January 4, 2010 (Perspective)
DOI: 10.1021/jm901361d
Abstract
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December 31, 2009

Urotensin-II Receptor Modulators as Potential Drugs

Bruce E. Maryanoff and William A. Kinney
Publication Date (Web): December 31, 2009 (Perspective)
DOI: 10.1021/jm901294u
Abstract
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December 14, 2009

Through the “Gatekeeper Door”: Exploiting the Active Kinase Conformation

Fabio Zuccotto, Elena Ardini, Elena Casale and Mauro Angiolini
Publication Date (Web): December 14, 2009 (Perspective)
DOI: 10.1021/jm901443h
Abstract
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December 10, 2009

Recent Advances in the Discovery of Competitive Protein Tyrosine Phosphatase 1B Inhibitors for the Treatment of Diabetes, Obesity, and Cancer

Andrew P. Combs
Publication Date (Web): December 10, 2009 (Perspective)
DOI: 10.1021/jm901090b
Abstract
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December 1, 2009

Selective p38α Inhibitors Clinically Evaluated for the Treatment of Chronic Inflammatory Disorders

David M. Goldstein, Andreas Kuglstatter, Yan Lou and Michael J. Soth
Publication Date (Web): December 1, 2009 (Perspective)
DOI: 10.1021/jm9012906
Abstract
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November 19, 2009

Perspectives of P-Glycoprotein Modulating Agents in Oncology and Neurodegenerative Diseases: Pharmaceutical, Biological, and Diagnostic Potentials

Nicola Antonio Colabufo, Francesco Berardi, Mariangela Cantore, Marialessandra Contino, Carmela Inglese, Mauro Niso and Roberto Perrone
Publication Date (Web): November 19, 2009 (Perspective)
DOI: 10.1021/jm900743c
Abstract
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October 29, 2009

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
Abstract | Supporting Info
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October 27, 2009

Selectively Nonselective Kinase Inhibition: Striking the Right Balance

Richard Morphy
Publication Date (Web): October 27, 2009 (Perspective)
DOI: 10.1021/jm901132v
Abstract
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Highlights in the Discovery of Antiviral Drugs: A Personal Retrospective

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