Table of Contents
April 24, 2003
Volume 46, Issue 9
Pages 1567-1774
Letters
The Pharmacophore of Short Cationic Antibacterial Peptides
Morten B. Strøm, Bengt Erik Haug, Merete L. Skar, Wenche Stensen, Trine Stiberg, and John S. Svendsen
pp 1567–1570Publication Date (Web): March 29, 2003 (Letter)
DOI: 10.1021/jm0340039
Hi-Res PDF Articles
Differential Binding Modes of Diacylglycerol (DAG) and DAG Lactones to Protein Kinase C (PK-C)
Dina M. Sigano, Megan L. Peach, Kassoum Nacro, Yongseok Choi, Nancy E. Lewin, Marc C. Nicklaus, Peter M. Blumberg, and Victor E. Marquez
pp 1571–1579Publication Date (Web): March 29, 2003 (Article)
DOI: 10.1021/jm020476o
Thyroid Receptor Ligands. 1. Agonist Ligands Selective for the Thyroid Receptor β1
Liu Ye, Yi-Lin Li, Karin Mellström, Charlotta Mellin, Lars-Göran Bladh, Konrad Koehler, Neeraj Garg, Ana Maria Garcia Collazo, Chris Litten, Bolette Husman, Karina Persson, Jan Ljunggren, Gary Grover, Paul G. Sleph, Rocco George, and Johan Malm
pp 1580–1588Publication Date (Web): March 21, 2003 (Article)
DOI: 10.1021/jm021080f
Bridged Bicyclic Cores Containing a 1,1-Diarylethylene Motif Are High-Affinity Subtype-Selective Ligands for the Estrogen Receptor
Rajeev S. Muthyala, Shubin Sheng, Kathryn E. Carlson, Benita S. Katzenellenbogen, and John. A. Katzenellenbogen
pp 1589–1602Publication Date (Web): April 2, 2003 (Article)
DOI: 10.1021/jm0204800
Tripeptide Probes for Tripeptidyl Protease I Production via Gene Transfer
MeeKyoung Kim, Qinwen Mao, Beverly L. Davidson, and David F. Wiemer
pp 1603–1608Publication Date (Web): March 29, 2003 (Article)
DOI: 10.1021/jm020525x
CoMFA and Homology-Based Models of the Glycine Binding Site of N-Methyl-d-aspartate Receptor
Irina G. Tikhonova, Igor I. Baskin, Vladimir A. Palyulin, and Nikolai S. Zefirov
pp 1609–1616Publication Date (Web): March 29, 2003 (Article)
DOI: 10.1021/jm0210156
Pharmacophore and Quantitative Structure−Activity Relationship Modeling: Complementary Approaches for the Rationalization and Prediction of UDP-Glucuronosyltransferase 1A4 Substrate Selectivity
Paul A. Smith, Michael J. Sorich, Ross A. McKinnon, and John O. Miners
pp 1617–1626Publication Date (Web): April 2, 2003 (Article)
DOI: 10.1021/jm020397c
Indole Naphthyridinones as Inhibitors of Bacterial Enoyl-ACP Reductases FabI and FabK
Mark A. Seefeld, William H. Miller, Kenneth A. Newlander, Walter J. Burgess, Walter E. DeWolfJr., Patricia A. Elkins, Martha S. Head, Dalia R. Jakas, Cheryl A. Janson, Paul M. Keller, Peter J. Manley, Terrance D. Moore, David J. Payne, Stewart Pearson, Brian J. Polizzi, Xiayang Qiu, Stephen F. Rittenhouse, Irene N. Uzinskas, Nicola G. Wallis, and William F. Huffman
pp 1627–1635Publication Date (Web): March 25, 2003 (Article)
DOI: 10.1021/jm0204035
An Ethylenamine Inhibitor Binds Tightly to Both Wild Type and Mutant HIV-1 Proteases. Structure and Energy Study
Tereza Skálová, Jindřich Hašek, Jan Dohnálek, Hana Petroková, Eva Buchtelová, and Jarmila DuškováMilan Souček, Pavel Majer, Táňa Uhlíková, and Jan Konvalinka
pp 1636–1644Publication Date (Web): March 29, 2003 (Article)
DOI: 10.1021/jm021079g
Construction and Assessment of Models of CYP2E1: Predictions of Metabolism from Docking, Molecular Dynamics, and Density Functional Theoretical Calculations
Jin-Young Park and Dan Harris
pp 1645–1660Publication Date (Web): March 29, 2003 (Article)
DOI: 10.1021/jm020538a
Aromatic Reduced Amide Bond Peptidomimetics as Selective Inhibitors of Neuronal Nitric Oxide Synthase
Jung-Mi Hah, Pavel Martásek, Linda J. Roman, and Richard B. Silverman
pp 1661–1669Publication Date (Web): March 29, 2003 (Article)
DOI: 10.1021/jm0202932
Synthesis, Anticancer Activity, and Inhibition of Tubulin Polymerization by Conformationally Restricted Analogues of Lavendustin A
Fanrong Mu, Ernest Hamel, Debbie J. Lee, Donald E. Pryor, and Mark Cushman
pp 1670–1682Publication Date (Web): April 02, 2003 (Article)
DOI: 10.1021/jm020292+
Full Text HTMLMitomycin Antitumor Compounds. 2. Interaction of Transition Metal Ions with Mitomycin C. Solution Structure and Biological Activity of a Pd2+−MMC Complex
Marina M. L. Fiallo, Eric Deydier, Michela Bracci, Arlette Garnier-Suillerot, and Karin Halvorsen
pp 1683–1689Publication Date (Web): March 29, 2003 (Article)
DOI: 10.1021/jm0209883
Self-Immolative Nitrogen Mustards Prodrugs Cleavable by Carboxypeptidase G2 (CPG2) Showing Large Cytotoxicity Differentials in GDEPT
Dan Niculescu-Duvaz, Ion Niculescu-Duvaz, Frank Friedlos, Jan Martin, Panos Lehouritis, Richard Marais, and Caroline J. Springer
pp 1690–1705Publication Date (Web): March 26, 2003 (Article)
DOI: 10.1021/jm020462i
Synthesis and Biological Evaluation of N-Heterocyclic Indolyl Glyoxylamides as Orally Active Anticancer Agents
Wen-Tai Li, Der-Ren Hwang, Ching-Ping Chen, Chien-Wei Shen, Chen-Long Huang, Tung-Wei Chen, Chi-Hung Lin, Yee-Ling Chang, Ying-Ying Chang, Yue-Kan Lo, Huan-Yi Tseng, Chu-Chung Lin, Jeng-Shin Song, Hua-Chien Chen, Shu-Jen Chen, Se−Hui Wu, and Chiung-Tong Chen
pp 1706–1715Publication Date (Web): March 25, 2003 (Article)
DOI: 10.1021/jm020471r
Comparison of in Vitro P-Glycoprotein Screening Assays: Recommendations for Their Use in Drug Discovery
Dietmar Schwab, Holger Fischer, Ali Tabatabaei, Sonia Poli, and Jörg Huwyler
pp 1716–1725Publication Date (Web): April 2, 2003 (Article)
DOI: 10.1021/jm021012t
Further Studies on 2,4-Diamino-5-(2‘,5‘-disubstituted benzyl)pyrimidines as Potent and Selective Inhibitors of Dihydrofolate Reductases from Three Major Opportunistic Pathogens of AIDS
Andre Rosowsky, Ronald A. Forsch, and Sherry F. Queener
pp 1726–1736Publication Date (Web): March 26, 2003 (Article)
DOI: 10.1021/jm020466n
Antitumor Activity of the Mixed Phosphine Gold Species Chlorotriphenylphosphine-1,3-bis(diphenylphosphino)propanegold(I)
Francesco Caruso, Miriam Rossi, Joseph Tanski, Claudio Pettinari, and Fabio Marchetti
pp 1737–1742Publication Date (Web): March 29, 2003 (Article)
DOI: 10.1021/jm0204690
New Cytotoxic and Water-Soluble Bis(2-phenylazopyridine)ruthenium(II) Complexes
Anna C. G. Hotze, Marina Bacac, Aldrik H. Velders, Bart A. J. Jansen, Huub Kooijman, Anthony L. Spek, Jaap G. Haasnoot, and Jan Reedijk
pp 1743–1750Publication Date (Web): March 25, 2003 (Article)
DOI: 10.1021/jm021110e
Solid-Phase Synthesis of Peptide Radiopharmaceuticals Using Fmoc-N-ε-(Hynic-Boc)−Lysine, a Technetium-Binding Amino Acid: Application to Tc-99m-Labeled Salmon Calcitonin
William E. P. Greenland, Kevin Howland, Judith Hardy, Ignac Fogelman, and Philip J. Blower
pp 1751–1757Publication Date (Web): March 27, 2003 (Article)
DOI: 10.1021/jm030761n
Synthesis and Biological Evaluation of 14-Alkoxymorphinans. 18.1 N-Substituted 14-Phenylpropyloxymorphinan-6-ones with Unanticipated Agonist Properties: Extending the Scope of Common Structure−Activity Relationships
Elisabeth Greiner, Mariana Spetea, Roland Krassnig, Falko Schüllner, Mario Aceto, Louis S. Harris, John R. Traynor, James H. Woods, Andrew Coop, and Helmut Schmidhammer
pp 1758–1763Publication Date (Web): March 29, 2003 (Article)
DOI: 10.1021/jm021118o
Brief Articles
Reduction of Peptide Character of HIV Protease Inhibitors That Exhibit Nanomolar Potency against Multidrug Resistant HIV-1 Strains
Hirokazu Tamamura, Yasuhiro Koh, Satoshi Ueda, Yoshikazu Sasaki, Tomonori Yamasaki, Manabu Aoki, Kenji Maeda, Yoriko Watai, Hisashi Arikuni, Akira Otaka, Hiroaki Mitsuya, and Nobutaka Fujii
pp 1764–1768Publication Date (Web): March 18, 2003 (Brief Article)
DOI: 10.1021/jm020537i
Design and Structure−Activity Relationships of 2-Alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl)imidazolo[1,2-a]pyrimid-5-ones as Potent GnRH Receptor Antagonists
Yun-Fei Zhu, Zhiqiang Guo, Timothy D. Gross, Yinghong Gao, Patrick J. Connors, Jr., R. Scott Struthers, Qiu Xie, Fabio C. Tucci, Greg J. Reinhart, Dongpei Wu, John Saunders, and Chen Chen
pp 1769–1772Publication Date (Web): March 28, 2003 (Brief Article)
DOI: 10.1021/jm0205402
Book Reviews
Combinatorial Library Methods and Protocols Edited by Lisa Bellavance English. Humana Press, Totowa, NJ. 2002. xi + 383 pp. 16 × 23.5 cm. ISBN 0-86093-980-3. $99.50.
Jan W. F. Wasley
p 1773Publication Date (Web): March 29, 2003 (Book Review)
DOI: 10.1021/jm030018v
Medicinal Chemistry: Principles and Practice. Second Edition Edited by F. D. King. The Royal Society of Chemistry, Cambridge, U.K. 2002. xxii + 450 pp. 15.5 × 23.5 cm. ISBN 0-85404-631-3(PB). £39.50.
Jonathan L. Vennerstrom
pp 1773–1774Publication Date (Web): March 18, 2003 (Book Review)
DOI: 10.1021/jm030058z