Journal of Medicinal Chemistry: Latest Articles (ACS Publications)

6-(Het)aryl-7-Deazapurine Ribonucleosides as Novel Potent Cytostatic Agents

Petr Nauš et al — Tue, 24 Nov 2009 20:40:07 GMT

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Carbamate Analogues of Fumagillin as Potent, Targeted Inhibitors of Methionine Aminopeptidase-2

Christopher C. Arico-Muendel et al — Tue, 24 Nov 2009 20:38:49 GMT

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Conformationally Constrained Mimetics of Laminin Peptide YIGSR as Precursors for Antimetastatic Disintegrins

Angelo Bella et al — Tue, 24 Nov 2009 20:37:01 GMT

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Biotin Derivatives Carrying Two Chelating DOTA Units. Synthesis, in Vitro Evaluation of Biotinidases Resistance, Avidin Binding, and Radiolabeling Tests

Alessandro Pratesi et al — Tue, 24 Nov 2009 16:09:05 GMT

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Potent and Orally Active Small-Molecule Inhibitors of the MDM2−p53 Interaction

Shanghai Yu et al — Tue, 24 Nov 2009 12:49:48 GMT

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Synthesis and Structure−Activity Studies of Biphenyl Analogues of the Tuberculosis Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824)

Brian D. Palmer et al — Tue, 24 Nov 2009 12:48:28 GMT

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Synthesis and Antiprotozoal Activity of Cationic 1,4-Diphenyl-1H-1,2,3-triazoles

Stanislav A. Bakunov et al — Mon, 23 Nov 2009 19:28:28 GMT

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Hybrid Inhibitors of Phosphatidylinositol 3-Kinase (PI3K) and the Mammalian Target of Rapamycin (mTOR): Design, Synthesis, and Superior Antitumor Activity of Novel Wortmannin−Rapamycin Conjugates

Semiramis Ayral-Kaloustian et al — Mon, 23 Nov 2009 17:14:03 GMT

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Synthesis and Opioid Receptor Binding Affinities of 2-Substituted and 3-Aminomorphinans: Ligands for μ, κ, and δ Opioid Receptors

Michael Decker et al — Mon, 23 Nov 2009 17:13:13 GMT

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Design of O-Acetylserine Sulfhydrylase Inhibitors by Mimicking Nature

Enea Salsi et al — Mon, 23 Nov 2009 17:11:29 GMT

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Displacement Assay for the Detection of Stabilizers of Inactive Kinase Conformations

Sabine Klüter et al — Mon, 23 Nov 2009 17:10:33 GMT

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Synthesis, Affinity Profile and Functional Activity of Potent Chiral Muscarinic Antagonists with a Pyrrolidinylfuran Structure†

Serena Scapecchi et al — Fri, 20 Nov 2009 15:18:53 GMT

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Novel Bisaryl Substituted Thiazoles and Oxazoles as Highly Potent and Selective Peroxisome Proliferator-Activated Receptor δ Agonists

Robert Epple et al — Fri, 20 Nov 2009 15:17:05 GMT

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9-Arylpurines as a Novel Class of Enterovirus Inhibitors

Leire Aguado et al — Thu, 19 Nov 2009 19:33:44 GMT

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X-ray Crystallographic Analysis of α-Ketoheterocycle Inhibitors Bound to a Humanized Variant of Fatty Acid Amide Hydrolase

Mauro Mileni et al — Thu, 19 Nov 2009 19:33:21 GMT

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

Nicola Antonio Colabufo et al — Thu, 19 Nov 2009 19:30:47 GMT

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The Structure−Activity Relationship of the Antimalarial Ozonide Arterolane (OZ277)

Yuxiang Dong et al — Thu, 19 Nov 2009 14:02:08 GMT

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Indol-3-ylcycloalkyl Ketones: Effects of N1 Substituted Indole Side Chain Variations on CB2 Cannabinoid Receptor Activity

Jennifer M. Frost et al — Wed, 18 Nov 2009 13:56:18 GMT

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Chloro-Substituted 3-Alkylamino-4H-1,2,4-benzothiadiazine 1,1-Dioxides as ATP-Sensitive Potassium Channel Activators: Impact of the Position of the Chlorine Atom on the Aromatic Ring on Activity and Tissue Selectivity

Bernard Pirotte et al — Wed, 18 Nov 2009 12:45:57 GMT

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Janus Kinase 2 Inhibitors. Synthesis and Characterization of a Novel Polycyclic Azaindole

Tiansheng Wang et al — Wed, 18 Nov 2009 12:45:53 GMT

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Identification of a Brain Penetrant PDE9A Inhibitor Utilizing Prospective Design and Chemical Enablement as a Rapid Lead Optimization Strategy

Patrick R. Verhoest et al — Tue, 17 Nov 2009 19:54:08 GMT

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Novel Organic Proteasome Inhibitors Identified by Virtual and in Vitro Screening

Nicolas Basse et al — Tue, 17 Nov 2009 15:08:08 GMT

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Structure-Based Design of Pteridine Reductase Inhibitors Targeting African Sleeping Sickness and the Leishmaniases

Lindsay B. Tulloch et al — Mon, 16 Nov 2009 19:54:58 GMT

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Morpholine Derivatives Greatly Enhance the Selectivity of Mammalian Target of Rapamycin (mTOR) Inhibitors

Arie Zask et al — Mon, 16 Nov 2009 15:20:17 GMT

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DNA Loop Sequence as the Determinant for Chiral Supramolecular Compound G-Quadruplex Selectivity

Haijia Yu et al — Fri, 13 Nov 2009 19:03:15 GMT

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Deciphering the Mechanism of Carbonic Anhydrase Inhibition with Coumarins and Thiocoumarins

Alfonso Maresca et al — Fri, 13 Nov 2009 19:02:04 GMT

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Structure−Activity Relationship Study of Betulinic Acid, A Novel and Selective TGR5 Agonist, and Its Synthetic Derivatives: Potential Impact in Diabetes¶

Cédric Genet et al — Fri, 13 Nov 2009 13:40:11 GMT

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Synthesis and Biological Evaluation of New Nanomolar Competitive Inhibitors of Helicobacter pylori Type II Dehydroquinase. Structural Details of the Role of the Aromatic Moieties with Essential Residues‡

Verónica F. V. Prazeres et al — Fri, 13 Nov 2009 13:39:36 GMT

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Discovery of 6α-Ethyl-23(S)-methylcholic Acid (S-EMCA, INT-777) as a Potent and Selective Agonist for the TGR5 Receptor, a Novel Target for Diabesity

Roberto Pellicciari et al — Thu, 12 Nov 2009 19:14:20 GMT

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Enhancement of the Antimalarial Activity of Ciprofloxacin Using a Double Prodrug/Bioorganometallic Approach

Faustine Dubar et al — Thu, 12 Nov 2009 19:14:04 GMT

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Quantitative Analyses of Aggregation, Autofluorescence, and Reactivity Artifacts in a Screen for Inhibitors of a Thiol Protease

Ajit Jadhav et al — Thu, 12 Nov 2009 16:52:47 GMT

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Dihydroxyphenylisoindoline Amides as Orally Bioavailable Inhibitors of the Heat Shock Protein 90 (Hsp90) Molecular Chaperone

Pei-Pei Kung et al — Thu, 12 Nov 2009 16:49:46 GMT

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Identification and Optimization of Inhibitors of Trypanosomal Cysteine Proteases: Cruzain, Rhodesain, and TbCatB

Bryan T. Mott et al — Thu, 12 Nov 2009 16:49:25 GMT

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

Shuangding Wu et al — Wed, 11 Nov 2009 16:08:23 GMT

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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 et al — Wed, 11 Nov 2009 16:05:59 GMT

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

Jalmira Mulchande et al — Wed, 11 Nov 2009 16:04:06 GMT

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

Arijit Das et al — Tue, 10 Nov 2009 20:05:47 GMT

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

Guo Li et al — Tue, 10 Nov 2009 19:10:12 GMT

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

Karen A. Evans et al — Tue, 10 Nov 2009 19:09:34 GMT

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

Nicolas Jullien et al — Mon, 09 Nov 2009 15:07:25 GMT

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Structural Studies of Pterin-Based Inhibitors of Dihydropteroate Synthase

Kirk E. Hevener et al — Mon, 09 Nov 2009 15:06:42 GMT

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The Discodermolide Hairpin Structure Flows from Conformationally Stable Modular Motifs

Ashutosh S. Jogalekar et al — Fri, 06 Nov 2009 18:31:48 GMT

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

François Maltais et al — Fri, 06 Nov 2009 12:58:20 GMT

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

Feng Liu et al — Thu, 05 Nov 2009 20:48:09 GMT

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

Fabrizio Micheli et al — Thu, 05 Nov 2009 20:29:11 GMT

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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 et al — Thu, 05 Nov 2009 15:47:45 GMT

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

Partha Pratim Bose et al — Thu, 05 Nov 2009 15:44:46 GMT

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Drug Effects Viewed from a Signal Transduction Network Perspective

Anton F. Fliri et al — Thu, 05 Nov 2009 15:42:32 GMT

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Structure−Activity Relationships of Polymyxin Antibiotics

Tony Velkov et al — Thu, 29 Oct 2009 19:27:38 GMT

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Selectively Nonselective Kinase Inhibition: Striking the Right Balance

Richard Morphy — Tue, 27 Oct 2009 17:04:12 GMT

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Highlights in the Discovery of Antiviral Drugs: A Personal Retrospective

Erik De Clercq — Tue, 27 Oct 2009 17:00:39 GMT

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

Hank F. Kung et al — Wed, 21 Oct 2009 19:25:43 GMT

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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 et al — Tue, 20 Oct 2009 17:22:45 GMT

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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 et al — Tue, 20 Oct 2009 17:22:18 GMT

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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 et al — Mon, 19 Oct 2009 15:46:53 GMT

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Three-Dimensional Pharmacophore Methods in Drug Discovery

Andrew R. Leach et al — Thu, 15 Oct 2009 14:36:53 GMT

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

Maria Laura Bolognesi et al — Thu, 08 Oct 2009 18:52:00 GMT

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

Marvin A. Soriano-Ursúa et al — Mon, 05 Oct 2009 18:12:30 GMT

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Imidazoquines as Antimalarial and Antipneumocystis Agents†

Nuno Vale et al — Fri, 02 Oct 2009 18:03:08 GMT

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

Sabine H. van Rijt et al — Wed, 30 Sep 2009 12:31:17 GMT

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

Lauren C. Purington et al — Tue, 29 Sep 2009 16:59:15 GMT

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

Claudio Biancalani et al — Tue, 29 Sep 2009 16:53:18 GMT

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

Youcef Mehellou et al — Mon, 28 Sep 2009 17:26:30 GMT

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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 et al — Thu, 24 Sep 2009 14:31:26 GMT

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

Thomas V. Magee et al — Wed, 23 Sep 2009 19:23:51 GMT

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

Philippe de Medina et al — Tue, 22 Sep 2009 12:37:23 GMT

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

Édith Bellavance et al — Tue, 22 Sep 2009 12:36:38 GMT

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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 et al — Mon, 21 Sep 2009 12:53:43 GMT

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

Vincenzo Tumiatti et al — Wed, 16 Sep 2009 17:39:38 GMT

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Mechanistic Insight into the Inhibition of Matrix Metalloproteinases by Platinum Substrates†

Fabio Arnesano et al — Wed, 16 Sep 2009 17:38:00 GMT

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Heat Shock Protein 90: Inhibitors in Clinical Trials

Marco A. Biamonte et al — Wed, 16 Sep 2009 16:54:28 GMT

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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 et al — Wed, 16 Sep 2009 11:40:37 GMT

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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 et al — Fri, 11 Sep 2009 19:34:03 GMT

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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 et al — Fri, 11 Sep 2009 18:48:09 GMT

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

Patrick M. Woster — Thu, 10 Sep 2009 18:20:25 GMT

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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 et al — Thu, 10 Sep 2009 18:14:14 GMT

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The Medicinal Chemistry of Dengue Fever

Andrew J. Stevens et al — Wed, 09 Sep 2009 17:28:08 GMT

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

Frederick W. Goldberg et al — Tue, 08 Sep 2009 13:19:32 GMT

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

Edward C. Lawson et al — Fri, 04 Sep 2009 19:31:41 GMT

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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 et al — Tue, 01 Sep 2009 16:02:46 GMT

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(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 et al — Thu, 03 Sep 2009 13:55:00 GMT

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

Enza Lacivita et al — Tue, 25 Aug 2009 19:43:40 GMT

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

Christian A. Olsen et al — Tue, 25 Aug 2009 17:29:37 GMT

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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 et al — Wed, 26 Aug 2009 15:35:55 GMT

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

Claudio Mapelli et al — Mon, 24 Aug 2009 15:34:12 GMT

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

Ashish P. Vartak et al — Wed, 19 Aug 2009 19:48:27 GMT

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

Lei Xiang Yang et al — Wed, 12 Aug 2009 14:27:19 GMT

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

Katiuscia Bonezzi et al — Mon, 10 Aug 2009 16:35:43 GMT

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

Rohit K. Sharma et al — Wed, 05 Aug 2009 18:08:20 GMT

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

Fabrizio Manetti et al — Mon, 03 Aug 2009 14:04:39 GMT

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

Jérôme Guillemont et al — Fri, 31 Jul 2009 19:30:17 GMT

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

Benoît Sanson et al — Thu, 30 Jul 2009 14:01:17 GMT

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Preclinical Efficacy of a Carboxylesterase 2-Activated Prodrug of Doxazolidine

Benjamin L. Barthel et al — Mon, 27 Jul 2009 18:07:59 GMT

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

Michael Decker et al — Mon, 27 Jul 2009 18:07:53 GMT

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Probes for Narcotic Receptor Mediated Phenomena. 39.(1) Enantiomeric N-Substituted Benzofuro[2,3-c]pyridin-6-ols: Synthesis and Topological Relationship to Oxide-Bridged Phenylmorphans(2)†

Yi Zhang et al — Fri, 24 Jul 2009 11:25:59 GMT

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

Bhaswati Sinha et al — Tue, 21 Jul 2009 13:08:31 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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 et al — Tue, 21 Jul 2009 13:08:12 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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

Igor Shamovsky et al — Fri, 17 Jul 2009 11:46:11 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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

Koushi Hidaka et al — Fri, 17 Jul 2009 11:45:49 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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

Giuseppe La Regina et al — Tue, 14 Jul 2009 15:43:04 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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

Andrea Cavalli et al — Thu, 16 Jul 2009 18:31:54 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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 et al — Wed, 08 Jul 2009 20:20:48 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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

Christian Peifer et al — Fri, 10 Jul 2009 17:47:32 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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

Nicolas Matuszak et al — Tue, 07 Jul 2009 20:09:12 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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 et al — Mon, 06 Jul 2009 16:38:22 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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

Claire S. Jacobs et al — Thu, 02 Jul 2009 14:44:35 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

Discovery of the First Series of Small Molecule H5N1 Entry Inhibitors

Gaopeng Song et al — Thu, 18 Jun 2009 13:13:42 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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 et al — Tue, 09 Jun 2009 18:46:13 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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

Zhao Dang et al — Mon, 15 Jun 2009 13:08:56 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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

Dilip K. Tosh et al — Mon, 08 Jun 2009 11:58:17 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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 et al — Thu, 23 Apr 2009 16:46:47 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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

Nareshkumar Jain et al — Tue, 14 Apr 2009 18:54:35 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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

Simone Di Micco et al — Fri, 23 Oct 2009 17:52:58 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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

S. Altieri et al — Fri, 30 Oct 2009 15:44:27 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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

Mei Yang et al — Fri, 06 Nov 2009 18:29:41 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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

Kui-Thong Tan et al — Fri, 06 Nov 2009 18:29:08 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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

Zheng Yin et al — Fri, 06 Nov 2009 18:28:29 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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 et al — Fri, 06 Nov 2009 18:31:13 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

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

Lauren Lee et al — Fri, 06 Nov 2009 12:58:31 GMT

Journal of Medicinal Chemistry, Volume 0, Issue 0, Articles ASAP (As Soon As Publishable).

Exploring Chemical Space with Aptamers

Michael Famulok — Thu, 19 Nov 2009 05:26:17 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 6951-6957, November 26, 2009.

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

David M. Bender et al — Thu, 19 Nov 2009 05:41:09 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 6958-6961, November 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 et al — Thu, 19 Nov 2009 05:40:53 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 6962-6965, November 26, 2009.

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

Jialin Mao et al — Thu, 19 Nov 2009 05:04:43 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 6966-6978, November 26, 2009.

Synthetic mRNA Splicing Modulator Compounds with in Vivo Antitumor Activity

Chandraiah Lagisetti et al — Thu, 19 Nov 2009 05:25:13 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 6979-6990, November 26, 2009.

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

Andreas Brust et al — Thu, 19 Nov 2009 05:43:15 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 6991-7002, November 26, 2009.

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

Bai He et al — Thu, 19 Nov 2009 05:28:22 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7003-7013, November 26, 2009.

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 et al — Thu, 19 Nov 2009 05:20:25 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7014-7028, November 26, 2009.

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

Vincent Rerat et al — Thu, 19 Nov 2009 05:45:48 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7029-7043, November 26, 2009.

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

John G. Allen et al — Thu, 19 Nov 2009 05:06:36 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7044-7053, November 26, 2009.

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

Marion Feledziak et al — Thu, 19 Nov 2009 05:14:08 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7054-7068, November 26, 2009.

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

Mirko Buchholz et al — Thu, 19 Nov 2009 05:05:10 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7069-7080, November 26, 2009.

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

Pawel Nowak et al — Thu, 19 Nov 2009 05:12:40 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7081-7089, November 26, 2009.

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

Kim Serdons et al — Thu, 19 Nov 2009 05:02:55 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7090-7102, November 26, 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 et al — Thu, 19 Nov 2009 05:44:43 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7103-7112, November 26, 2009.

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

Padraic S. Nagle et al — Thu, 19 Nov 2009 05:03:18 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7113-7121, November 26, 2009.

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 et al — Thu, 19 Nov 2009 05:02:25 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7122-7131, November 26, 2009.

Design of HIV Protease Inhibitors Based on Inorganic Polyhedral Metallacarboranes

Pavlína Řezáčová et al — Thu, 19 Nov 2009 05:09:29 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7132-7141, November 26, 2009.

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

Karen A. Nolan et al — Thu, 19 Nov 2009 05:13:37 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7142-7156, November 26, 2009.

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 et al — Thu, 19 Nov 2009 05:41:31 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7157-7162, November 26, 2009.

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

Dai-Shi Su et al — Thu, 19 Nov 2009 05:12:11 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7163-7169, November 26, 2009.

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 et al — Thu, 19 Nov 2009 05:08:16 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7170-7185, November 26, 2009.

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

Nathalie Schlienger et al — Thu, 19 Nov 2009 05:40:32 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7186-7191, November 26, 2009.

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

Asli Ovat et al — Thu, 19 Nov 2009 05:23:27 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7192-7210, November 26, 2009.

Azaindole Hydroxamic Acids are Potent HIV-1 Integrase Inhibitors

Michael B. Plewe et al — Thu, 19 Nov 2009 05:11:30 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7211-7219, November 26, 2009.

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

Gonzalo García et al — Thu, 19 Nov 2009 05:19:28 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7220-7227, November 26, 2009.

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 et al — Thu, 19 Nov 2009 05:45:11 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7228-7235, November 26, 2009.

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

Dan Kaufmann et al — Thu, 19 Nov 2009 05:17:39 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7236-7248, November 26, 2009.

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

Mariana P. Arce et al — Thu, 19 Nov 2009 05:12:56 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7249-7257, November 26, 2009.

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 et al — Thu, 19 Nov 2009 05:42:16 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7258-7272, November 26, 2009.

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

Paola Failli et al — Thu, 19 Nov 2009 05:07:17 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7273-7283, November 26, 2009.

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

Toshimitsu Okamura et al — Thu, 19 Nov 2009 05:08:43 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7284-7288, November 26, 2009.

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

Takashi Mizutani et al — Thu, 19 Nov 2009 05:11:10 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7289-7300, November 26, 2009.

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

F. Ivy Carroll et al — Thu, 19 Nov 2009 05:11:48 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7301-7309, November 26, 2009.

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

Coco N. Kapanda et al — Thu, 19 Nov 2009 05:27:48 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7310-7314, November 26, 2009.

Novel Compounds Designed as Antistress Agents

Karyophyllis C. Tsiakitzis et al — Thu, 19 Nov 2009 05:07:51 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7315-7318, November 26, 2009.

Might Adrenergic α2C-Agonists/α2A-Antagonists Become Novel Therapeutic Tools for Pain Treatment with Morphine?(1)

Claudia Cardinaletti et al — Thu, 19 Nov 2009 05:00:53 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7319-7322, November 26, 2009.

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

Masako Okamoto et al — Thu, 19 Nov 2009 05:15:32 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7323-7327, November 26, 2009.

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

Jessica J. Field et al — Thu, 19 Nov 2009 05:18:12 GMT

Journal of Medicinal Chemistry, Volume 52, Issue 22, Page 7328-7332, November 26, 2009.