Table of Contents
July 15, 2004
Volume 47, Issue 15
Pages 3707-3896
About the Cover: Ribbon rendered illustration of the nuclear receptor heterodimer RXRα(cyan):PPARRγ (red) ligand binding domains bound with coactivator peptides (magenta) and agonist ligands (space-filling atoms where green is carbon, red is oxygen, and blue is nitrogen) (Haffner, C. D.; et al. J. Med. Chem. 2004, 47, 2010-2029).
Letters
New, Non-Adenosine, High-Potency Agonists for the Human Adenosine A2B Receptor with an Improved Selectivity Profile Compared to the Reference Agonist N-Ethylcarboxamidoadenosine
Margot W. Beukers, Lisa C. W. Chang, Jacobien K. von Frijtag Drabbe Künzel, Thea Mulder-Krieger, Ronald F. Spanjersberg, Johannes Brussee, and Ad P. IJzerman
pp 3707–3709Publication Date (Web): June 15, 2004 (Letter)
DOI: 10.1021/jm049947s
Hi-Res PDF Articles
N2-Substituted O6-Cyclohexylmethylguanine Derivatives: Potent Inhibitors of Cyclin-Dependent Kinases 1 and 2
Ian R. Hardcastle, Christine E. Arris, Johanne Bentley, F. Thomas Boyle, Yuzhu Chen, Nicola J. Curtin, Jane A. Endicott, Ashleigh E. Gibson, Bernard T. Golding, Roger J. Griffin, Philip Jewsbury, Jerome Menyerol, Veronique Mesguiche, David R. Newell, Martin E. M. Noble, David J. Pratt, Lan-Zhen Wang, and Hayley J. Whitfield
pp 3710–3722Publication Date (Web): June 10, 2004 (Article)
DOI: 10.1021/jm0311442
A Common Pharmacophoric Footprint for AIDS Vaccine Design
Christoph Pisterer, Dan Mihailescu, Jeremy C. Smith, and Jennifer Reed
pp 3723–3729Publication Date (Web): June 18, 2004 (Article)
DOI: 10.1021/jm031125s
Structure-Based Design, Synthesis, and Structure−Activity Relationship Studies of Novel Non-nucleoside Adenosine Deaminase Inhibitors
Tadashi Terasaka, Takayoshi Kinoshita, Masako Kuno, Nobuo Seki, Kohichiro Tanaka, and Isao Nakanishi
pp 3730–3743Publication Date (Web): June 17, 2004 (Article)
DOI: 10.1021/jm0306374
Pyridinium Cationic Lipids in Gene Delivery: A Structure−Activity Correlation Study
Marc Antoniu Ilies, William A. Seitz, Ion Ghiviriga, Betty H. Johnson, Aaron Miller, E. Brad Thompson, and Alexandru T. Balaban
pp 3744–3754Publication Date (Web): June 19, 2004 (Article)
DOI: 10.1021/jm0499763
Rational Design of New Antituberculosis Agents: Receptor-Independent Four-Dimensional Quantitative Structure−Activity Relationship Analysis of a Set of Isoniazid Derivatives
Kerly F. M. Pasqualoto, Elizabeth I. Ferreira, Osvaldo A. Santos-Filho, and Anton J. Hopfinger
pp 3755–3764Publication Date (Web): June 12, 2004 (Article)
DOI: 10.1021/jm049913k
A Ligand-Based Approach To Identify Quantitative Structure−Activity Relationships for the Androgen Receptor
Casey E. Bohl, Cheng Chang, Michael L. Mohler, Jiyun Chen, Duane D. Miller, Peter W. Swaan, and James T. Dalton
pp 3765–3776Publication Date (Web): June 19, 2004 (Article)
DOI: 10.1021/jm0499007
Pruned Receptor Surface Models and Pharmacophores for Three-Dimensional Database Searching
Jeffrey J. Sutherland, Lee A. O'Brien, and Donald F. Weaver
pp 3777–3787Publication Date (Web): June 17, 2004 (Article)
DOI: 10.1021/jm049896z
Novel Azapeptide Inhibitors of Hepatitis C Virus Serine Protease
Murray D. Bailey, Ted Halmos, Nathalie Goudreau, Ewen Lescop, and Montse Llinàs-Brunet
pp 3788–3799Publication Date (Web): June 17, 2004 (Article)
DOI: 10.1021/jm049864b
Synthesis and Antitumor Activity of Quinonoid Derivatives of Cannabinoids
Natalya M. Kogan, Ruth Rabinowitz, Paloma Levi, Dan Gibson, Peter Sandor, Michael Schlesinger, and Raphael Mechoulam
pp 3800–3806Publication Date (Web): June 10, 2004 (Article)
DOI: 10.1021/jm040042o
PDBLIG: Classification of Small Molecular Protein Binding in the Protein Data Bank
Andrew J. Chalk, Catherine L. Worth, John P. Overington, and A. W. Edith Chan
pp 3807–3816Publication Date (Web): June 19, 2004 (Article)
DOI: 10.1021/jm040804f
Novel S-Substituted Aminoalkylamino Ethanethiols as Potential Antidotes against Sulfur Mustard Toxicity
Uma Pathak, Syed K. Raza, A. S. Kulkarni, Rajagopalan Vijayaraghvan, Pravin Kumar, and Devendra K. Jaiswal
pp 3817–3822Publication Date (Web): June 19, 2004 (Article)
DOI: 10.1021/jm030099v
Studies toward the Discovery of the Next Generation of Antidepressants. 3. Dual 5-HT1A and Serotonin Transporter Affinity within a Class of N-Aryloxyethylindolylalkylamines
Richard E. Mewshaw, Dahui Zhou, Ping Zhou, Xiaojie Shi, Geoffrey Hornby, Taylor Spangler, Rosemary Scerni, Deborah Smith, Lee E. Schechter, and Terrance H. Andree
pp 3823–3842Publication Date (Web): June 17, 2004 (Article)
DOI: 10.1021/jm0304010
Sulfonyl-Containing Aldophosphamide Analogues as Novel Anticancer Prodrugs Targeted against Cyclophosphamide-Resistant Tumor Cell Lines
Monish Jain, Junying Fan, Nesrine Z. Baturay, and Chul-Hoon Kwon
pp 3843–3852Publication Date (Web): June 17, 2004 (Article)
DOI: 10.1021/jm0304764
Discovery of 2-(4-Pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a Dopaminergic Agent with a Novel Mode of Action for the Potential Treatment of Erectile Dysfunction
Marlon Cowart, Steven P. Latshaw, Pramila Bhatia, Jerome F. Daanen, Jeffrey Rohde, Sherry L. Nelson, Meena Patel, Teodozyi Kolasa, Masaki Nakane, Marie E. Uchic, Loan N. Miller, Marc A. Terranova, Renjie Chang, Diana L. Donnelly-Roberts, Marian T. Namovic, Peter R. Hollingsworth, Brenda R. Martino, James J. Lynch, III, James P. Sullivan, Gin C. Hsieh, Robert B. Moreland, Jorge D. Brioni, and Andrew O. Stewart
pp 3853–3864Publication Date (Web): June 10, 2004 (Article)
DOI: 10.1021/jm030505a
Synthesis and Biological Evaluation of a New Class of Geldanamycin Derivatives as Potent Inhibitors of Hsp90
Jean-Yves Le Brazidec, Adeela Kamal, David Busch, Lia Thao, Lin Zhang, Gregg Timony, Roy Grecko, Katy Trent, Rachel Lough, Tim Salazar, Samina Khan, Francis Burrows, and Marcus F. Boehm
pp 3865–3873Publication Date (Web): June 17, 2004 (Article)
DOI: 10.1021/jm0306125
Synthesis and Biological Evaluation of 2-Phenylpyran-4-ones: A New Class of Orally Active Cyclooxygenase-2 Inhibitors
Francisco Caturla, Juan-Miguel Jiménez, Núria Godessart, Mercè Amat, Alvaro Cárdenas, Lídia Soca, Jordi Beleta, Hamish Ryder, and María I. Crespo
pp 3874–3886Publication Date (Web): June 17, 2004 (Article)
DOI: 10.1021/jm049882t
2-Amino-O4-benzylpteridine Derivatives: Potent Inactivators of O6-Alkylguanine-DNA Alkyltransferase
Michael E. Nelson, Natalia A. Loktionova, Anthony E. Pegg, and Robert C. Moschel
pp 3887–3891Publication Date (Web): June 18, 2004 (Article)
DOI: 10.1021/jm049758+
Full Text HTML Brief Articles
Simple, Short Peptide Derivatives of a Sulfonylindolecarboxamide (L-737,126) Active in Vitro against HIV-1 Wild Type and Variants Carrying Non-Nucleoside Reverse Transcriptase Inhibitor Resistance Mutations
Romano Silvestri, Marino Artico, Gabriella De Martino, Giuseppe La Regina, Roberta Loddo, Massimiliano La Colla, and Paolo La Colla
pp 3892–3896Publication Date (Web): June 22, 2004 (Brief Article)
DOI: 10.1021/jm031147e