Table of Contents
July 14, 2005
Volume 48, Issue 14
Pages 4491-4703
About the Cover: Illustration of the binding mode of a biheteroaryl inhibitor to vascular endothelial growth factor receptor-2 (Kuo, G.-H.; et al. J. Med. Chem. 2005, 48, 1886-1900).
Perspective
p53 Activation by Small Molecules: Application in Oncology
Lyubomir T. Vassilev
pp 4491–4499Publication Date (Web): June 18, 2005 (Perspective)
DOI: 10.1021/jm058174k
Hi-Res PDF Letters
[Nα-BenzylTyr1,cyclo(d-Asp5,Dap8)]- dynorphin A-(1−11)NH2 Cyclized in the “Address” Domain Is a Novel κ-Opioid Receptor Antagonist
Kshitij A. Patkar, Xiuzhen Yan, Thomas F. Murray, and Jane V. Aldrich
pp 4500–4503Publication Date (Web): June 15, 2005 (Letter)
DOI: 10.1021/jm050105i
Highly Stable Phenanthridinium Frameworks as a New Class of Tunable DNA Binding Agents with Cytotoxic Properties
Alexis D. C. Parenty, Louise V. Smith, Kevin M. Guthrie, De-Liang Long, Jane Plumb, Robert Brown, and Leroy Cronin
pp 4504–4506Publication Date (Web): June 17, 2005 (Letter)
DOI: 10.1021/jm050320z
Design and Synthesis of New Nonsteroidal Glucocorticoid Modulators through Application of an “Agreement Docking” Method
Mike Barker, Margaret Clackers, Derek A. Demaine, Davina Humphreys, Michael J. Johnston, Haydn T. Jones, Francois Pacquet, John M. Pritchard, Mark Salter, Stephen E. Shanahan, Philip A. Skone, Victoria M. Vinader, Iain Uings, Iain M. McLay, and Simon J. F. Macdonald
pp 4507–4510Publication Date (Web): June 16, 2005 (Letter)
DOI: 10.1021/jm050345y
Articles
Probing the Subpockets of Factor Xa Reveals Two Binding Modes for Inhibitors Based on a 2-Carboxyindole Scaffold: A Study Combining Structure-Activity Relationship and X-ray Crystallography
Marc Nazaré, David W. Will, Hans Matter, Herman Schreuder, Kurt Ritter, Matthias Urmann, Melanie Essrich, Armin Bauer, Michael Wagner, Jörg Czech, Martin Lorenz, Volker Laux, and Volkmar Wehner
pp 4511–4525Publication Date (Web): June 11, 2005 (Article)
DOI: 10.1021/jm0490540
Synthesis and Biological Evaluation of Geminal Disulfones as HIV-1 Integrase Inhibitors
D. Christopher Meadows, Timothy B. Mathews, Thomas W. North, Michael J. Hadd, Chih Lin Kuo, Nouri Neamati, and Jacquelyn Gervay-Hague
pp 4526–4534Publication Date (Web): June 14, 2005 (Article)
DOI: 10.1021/jm049171v
Synthesis and Identification of [1,3,5]Triazine-pyridine Biheteroaryl as a Novel Series of Potent Cyclin-Dependent Kinase Inhibitors
Gee-Hong Kuo, Alan DeAngelis, Stuart Emanuel, Aihua Wang, Yan Zhang, Peter J. Connolly, Xin Chen, Robert H. Gruninger, Catherine Rugg, Angel Fuentes-Pesquera, Steven A. Middleton, Linda Jolliffe, and William V. Murray
pp 4535–4546Publication Date (Web): May 27, 2005 (Article)
DOI: 10.1021/jm040214h
Potent Inhibitors of Subgenomic Hepatitis C Virus RNA Replication through Optimization of Indole-N-Acetamide Allosteric Inhibitors of the Viral NS5B Polymerase
Steven Harper, Salvatore Avolio, Barbara Pacini, Marcello Di Filippo, Sergio Altamura, Licia Tomei, Giacomo Paonessa, Stefania Di Marco, Andrea Carfi, Claudio Giuliano, Julio Padron, Fabio Bonelli, Giovanni Migliaccio, Raffaele De Francesco, Ralph Laufer, Michael Rowley, and Frank Narjes
pp 4547–4557Publication Date (Web): June 11, 2005 (Article)
DOI: 10.1021/jm050056+
Full Text HTMLLarge-Scale Validation of a Quantum Mechanics Based Scoring Function: Predicting the Binding Affinity and the Binding Mode of a Diverse Set of Protein−Ligand Complexes
Kaushik Raha and Kenneth M. Merz, Jr.
pp 4558–4575Publication Date (Web): June 21, 2005 (Article)
DOI: 10.1021/jm048973n
Adamantyl Cannabinoids: A Novel Class of Cannabinergic Ligands
Dai Lu, Zhaoxing Meng, Ganesh A. Thakur, Pusheng Fan, John Steed, Cindy L. Tartal, Dow P. Hurst, Patricia H. Reggio, Jeffrey R. Deschamps, Damon A. Parrish, Clifford George, Torbjörn U. C. Järbe, Richard J. Lamb, and Alexandros Makriyannis
pp 4576–4585Publication Date (Web): June 16, 2005 (Article)
DOI: 10.1021/jm058175c
Identification of Novel Extracellular Signal-Regulated Kinase Docking Domain Inhibitors
Chad N. Hancock, Alba Macias, Eun Kyoung Lee, Su Yeon Yu, Alexander D. MacKerell, Jr., and Paul Shapiro
pp 4586–4595Publication Date (Web): June 21, 2005 (Article)
DOI: 10.1021/jm0501174
Design and Synthesis of the First Generation of Novel Potent, Selective, and in Vivo Active (Benzothiazol-2-yl)acetonitrile Inhibitors of the c-Jun N-Terminal Kinase
Pascale Gaillard, Isabelle Jeanclaude-Etter, Vittoria Ardissone, Steve Arkinstall, Yves Cambet, Montserrat Camps, Christian Chabert, Dennis Church, Rocco Cirillo, Denise Gretener, Serge Halazy, Anthony Nichols, Cedric Szyndralewiez, Pierre-Alain Vitte, and Jean-Pierre Gotteland
pp 4596–4607Publication Date (Web): June 09, 2005 (Article)
DOI: 10.1021/jm0310986
Synthesis and Immunosuppressive Activity of New Artemisinin Derivatives. 1. [12(β or α)-Dihydroartemisininoxy]phen(ox)yl Aliphatic Acids and Esters
Zhong-Shun Yang, Wen-Liang Zhou, Yi Sui, Jun-Xia Wang, Jin-Ming Wu, Yu Zhou, Yu Zhang, Pei-Lan He, Ji-Ye Han, Wei Tang, Ying Li, and Jian-Ping Zuo
pp 4608–4617Publication Date (Web): June 14, 2005 (Article)
DOI: 10.1021/jm048979c
Novel α-Amino-3-hydroxy-5-methyl-4-isoxazole Propionate (AMPA) Receptor Antagonists of 2,3-Benzodiazepine Type: Chemical Synthesis, in Vitro Characterization, and in Vivo Prevention of Acute Neurodegeneration
Bernd Elger, Andreas Huth, Roland Neuhaus, Eckard Ottow, Herbert Schneider, Bernd Seilheimer, and Lechoslaw Turski
pp 4618–4627Publication Date (Web): June 21, 2005 (Article)
DOI: 10.1021/jm0580003
Synthesis and Structure−Activity Relationships of Soluble 7-Substituted 3-(3,5-Dimethoxyphenyl)-1,6-naphthyridin-2-amines and Related Ureas as Dual Inhibitors of the Fibroblast Growth Factor Receptor-1 and Vascular Endothelial Growth Factor Receptor-2 Tyrosine Kinases
Andrew M. Thompson, Amy M. Delaney, James M. Hamby, Mel C. Schroeder, Teresa A. Spoon, Sheila M. Crean, H. D. Hollis Showalter, and William A. Denny
pp 4628–4653Publication Date (Web): June 17, 2005 (Article)
DOI: 10.1021/jm0500931
Potent Androgen Antagonists Based on Carborane as a Hydrophobic Core Structure
Shinya Fujii, Tokuhito Goto, Kiminori Ohta, Yuichi Hashimoto, Tomoharu Suzuki, Shigeru Ohta, and Yasuyuki Endo
pp 4654–4662Publication Date (Web): June 17, 2005 (Article)
DOI: 10.1021/jm050115j
The Taming of Capsaicin. Reversal of the Vanilloid Activity of N-Acylvanillamines by Aromatic Iodination
Giovanni Appendino, Nives Daddario, Alberto Minassi, Aniello Schiano Moriello, Luciano De Petrocellis, and Vincenzo Di Marzo
pp 4663–4669Publication Date (Web): June 10, 2005 (Article)
DOI: 10.1021/jm050139q
Selective Substrate-Based Inhibitors of Mammalian Dimethylarginine Dimethylaminohydrolase
Sharon Rossiter, Caroline L. Smith, Mohammed Malaki, Manasi Nandi, Herpreet Gill, James M. Leiper, Patrick Vallance, and David L. Selwood
pp 4670–4678Publication Date (Web): June 14, 2005 (Article)
DOI: 10.1021/jm050187a
Second Generation Transition State Analogue Inhibitors of Human 5‘-Methylthioadenosine Phosphorylase
Gary B. Evans, Richard H. Furneaux, Dirk H. Lenz, Gavin F. Painter, Vern L. Schramm, Vipender Singh, and Peter C. Tyler
pp 4679–4689Publication Date (Web): June 21, 2005 (Article)
DOI: 10.1021/jm050269z
Synthesis and Biological Evaluation of Acyclic 3-[(2-Hydroxyethoxy)methyl] Analogues of Antiviral Furo- and Pyrrolo[2,3-d]pyrimidine Nucleosides1
Zlatko Janeba, Jan Balzarini, Graciela Andrei, Robert Snoeck, Erik De Clercq, and Morris J. Robins
pp 4690–4696Publication Date (Web): June 21, 2005 (Article)
DOI: 10.1021/jm050291s
Brief Articles
New Pyrrolo[2,1-f]purine-2,4-dione and Imidazo[2,1-f]purine-2,4-dione Derivatives as Potent and Selective Human A3 Adenosine Receptor Antagonists
Pier Giovanni Baraldi, Delia Preti, Mojgan Aghazadeh Tabrizi, Francesca Fruttarolo, Romeo Romagnoli, Naser Abdel Zaid, Allan R. Moorman, Stefania Merighi, Katia Varani, and Pier Andrea Borea
pp 4697–4701Publication Date (Web): June 21, 2005 (Brief Article)
DOI: 10.1021/jm058008c
Book Reviews
p 4702
Publication Date (Web): June 21, 2005 (Book Review)
DOI: 10.1021/jm058233u
Additions and Corrections
Architecture of the Human Urotensin II Receptor: Comparison of the Binding Domains of Peptide and Non-Peptide Urotensin II Agonists.
Antonio Lavecchia, Sandro Cosconati, and Ettore Novellino:
p 4703Publication Date (Web): June 11, 2005 (Addition/Correction)
DOI: 10.1021/jm058024+