Table of Contents
April 11, 2002
Volume 45, Issue 8
Pages 1543-1735
Perspectives
Inhibition of Protein−Protein Association by Small Molecules: Approaches and Progress
Peter L. Toogood
pp 1543–1558Publication Date (Web): March 15, 2002 (Perspective)
DOI: 10.1021/jm010468s
Letters
Biological Activity of the Tryprostatins and Their Diastereomers on Human Carcinoma Cell Lines
Shuo Zhao, Kirsten S. Smith, Amy Morin Deveau, Christine M. Dieckhaus, Michael A. Johnson, Timothy L. Macdonald, and James M. Cook
pp 1559–1562Publication Date (Web): March 15, 2002 (Letter)
DOI: 10.1021/jm0155953
β-C-Mannosides as Selectin Inhibitors
Neelu Kaila, Lihren Chen, Bert E. Thomas IV, Desiree Tsao, Steve Tam, Patricia W. Bedard, Raymond T. Camphausen, Juan C. Alvarez, and Giliyar Ullas
pp 1563–1566Publication Date (Web): March 14, 2002 (Letter)
DOI: 10.1021/jm010390f
Articles
Synthesis, Biological Evaluation, and Binding Mode of Novel 1-[2-(Diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles Targeted at the HIV-1 Reverse Transcriptase
Romano Silvestri, Marino Artico, Gabriella De Martino, Rino Ragno, Silvio Massa, Roberta Loddo, Chiara Murgioni, Anna Giulia Loi, Paolo La Colla, and Alessandra Pani
pp 1567–1576Publication Date (Web): March 07, 2002 (Article)
DOI: 10.1021/jm010904a
GBR Compounds and Mepyramines as Cocaine Abuse Therapeutics: Chemometric Studies on Selectivity Using Grid Independent Descriptors (GRIND)
Paolo Benedetti, Raimund Mannhold, Gabriele Cruciani, and Manuel Pastor
pp 1577–1584Publication Date (Web): March 08, 2002 (Article)
DOI: 10.1021/jm011007+
Development of New Hydrogen-Bond Descriptors and Their Application to Comparative Molecular Field Analyses
Markus Böhm and Gerhard Klebe
pp 1585–1597Publication Date (Web): March 16, 2002 (Article)
DOI: 10.1021/jm011039x
Novel Approach for Linking Genotype to Phenotype in Vitro by Exploiting an Extremely Strong Interaction between RNA and Protein
Satoshi Fujita, Shinya Y. Sawata, Rika Yamamoto-Fujita, Yaeta Endo, Hideo Kise, Masahiro Iwakura, and Kazunari Taira
pp 1598–1606Publication Date (Web): March 07, 2002 (Article)
DOI: 10.1021/jm010398p
Structure-Based Design, Synthesis, and Biological Evaluation of Irreversible Human Rhinovirus 3C Protease Inhibitors. 6. Structure−Activity Studies of Orally Bioavailable, 2-Pyridone-Containing Peptidomimetics
Peter S. Dragovich, Thomas J. Prins, Ru Zhou, Edward L. Brown, Fausto C. Maldonado, Shella A. Fuhrman, Leora S. Zalman, Tove Tuntland, Caroline A. Lee, Amy K. Patick, David A. Matthews, Thomas F. Hendrickson, Maha B. Kosa, Bo Liu, Minerva R. Batugo, Jean-Paul R. Gleeson, Sylvie K. Sakata, Lijian Chen, Mark C. Guzman, James W. Meador, III, Rose Ann Ferre, and Stephen T. Worland
pp 1607–1623Publication Date (Web): March 08, 2002 (Article)
DOI: 10.1021/jm010469k
Bioactive Pseudopeptidic Analogues and Cyclostereoisomers of Osteogenic Growth Peptide C-Terminal Pentapeptide, OGP(10−14)
Yu-Chen Chen, Andras Muhlrad, Arie Shteyer, Marina Vidson, Itai Bab, and Michael Chorev
pp 1624–1632Publication Date (Web): March 15, 2002 (Article)
DOI: 10.1021/jm010479l
Structure−Activity Relationships in 1,4-Benzodioxan-Related Compounds. 7.1 Selectivity of 4-Phenylchroman Analogues for α1−Adrenoreceptor Subtypes
Wilma Quaglia, Maria Pigini, Alessandro Piergentili, Mario Giannella, Francesco Gentili, Gabriella Marucci, Antonio Carrieri, Angelo Carotti, Elena Poggesi, Amedeo Leonardi, and Carlo Melchiorre
pp 1633–1643Publication Date (Web): March 12, 2002 (Article)
DOI: 10.1021/jm011066n
Design, Synthesis, and Structure−Activity Relationship of Pyridyl Imidazolidinones: A Novel Class of Potent and Selective Human Enterovirus 71 Inhibitors
Kak-Shan Shia, Wen-Tai Li, Chung-Ming Chang, Ming-Chu Hsu, Jyh-Haur Chern, Max K. Leong, Sung-Nien Tseng, Chung-Chi Lee, Yen-Chun Lee, Shu-Jen Chen, Kuan-Chang Peng, Huan-Yi Tseng, Yi-Ling Chang, Chia-Liang Tai, and Shin-Ru Shih
pp 1644–1655Publication Date (Web): March 13, 2002 (Article)
DOI: 10.1021/jm010536a
Geometry−Affinity Relationships of the Selective Serotonin Receptor Ligand 9-(Aminomethyl)-9,10-dihydroanthracene
Scott P. Runyon, Srinivas Peddi, Jason E. Savage, Bryan L. Roth, Richard A. Glennon, and Richard B. Westkaemper
pp 1656–1664Publication Date (Web): March 15, 2002 (Article)
DOI: 10.1021/jm010354g
Human Somatostatin Receptor Specificity of Backbone-Cyclic Analogues Containing Novel Sulfur Building Units
Sharon Gazal, Garry Gelerman, Ofer Ziv, Olga Karpov, Pninit Litman, Moshe Bracha, Michel Afargan, and Chaim Gilon
pp 1665–1671Publication Date (Web): March 16, 2002 (Article)
DOI: 10.1021/jm0100281
Gold(III) Complexes with Bipyridyl Ligands: Solution Chemistry, Cytotoxicity, and DNA Binding Properties
Giordana Marcon, Stefania Carotti, Marcella Coronnello, Luigi Messori, Enrico Mini, Pierluigi Orioli, Teresita Mazzei, Maria Agostina Cinellu, and Giovanni Minghetti
pp 1672–1677Publication Date (Web): March 13, 2002 (Article)
DOI: 10.1021/jm010997w
Synthesis of Photoreactive Phosphatidic Acid Analogues Displaying Activatory Properties on Cyclic AMP-phosphodiesterases. Photoaffinity Labeling of an Isoform of Phosphodiesterase
Madeleine Picq, Yan Huang, Michel Lagarde, Alain Doutheau, and Georges Nemoz
pp 1678–1685Publication Date (Web): March 12, 2002 (Article)
DOI: 10.1021/jm011032f
Synthesis and Biological Characterization of L-N6-(1-Iminoethyl)lysine 5-Tetrazole-amide, a Prodrug of a Selective iNOS Inhibitor
E. Ann Hallinan, Sofya Tsymbalov, Clifford R. Dorn, Barnett S. Pitzele, and Donald W. Hansen, Jr.William M. Moore, Gina M. Jerome, Jane R. Connor, Linda F. Branson, Deborah L. Widomski, Yan Zhang, Mark G. Currie, and Pamela T. Manning
pp 1686–1689Publication Date (Web): March 13, 2002 (Article)
DOI: 10.1021/jm010420e
Synthesis and In Vitro Antitumor Activity of New Deaza Analogues of the Nonpolyglutamatable Antifolate Nα-(4-Amino-4-deoxypteroyl)-Nδ-hemiphthaloyl-l-ornithine (PT523)
Chitra M. Vaidya, Joel E. Wright, and Andre Rosowsky
pp 1690–1696Publication Date (Web): March 16, 2002 (Article)
DOI: 10.1021/jm010518t
Potent, Orally Active Heterocycle-Based Combretastatin A-4 Analogues: Synthesis, Structure−Activity Relationship, Pharmacokinetics, and In Vivo Antitumor Activity Evaluation
Le Wang, Keith W. Woods, Qun Li, Kenneth J. Barr, Richard W. McCroskey, Steven M. Hannick, Laura Gherke, R. Bruce Credo, Yu-Hua Hui, Kennan Marsh, Robert Warner, Jang Y. Lee, Nicolette Zielinski-Mozng, David Frost, Saul H. Rosenberg, and Hing L. Sham
pp 1697–1711Publication Date (Web): March 13, 2002 (Article)
DOI: 10.1021/jm010523x
A Common Mechanism Underlying Promiscuous Inhibitors from Virtual and High-Throughput Screening
Susan L. McGovern, Emilia Caselli, Nikolaus Grigorieff, and Brian K. Shoichet
pp 1712–1722Publication Date (Web): March 09, 2002 (Article)
DOI: 10.1021/jm010533y
Conceptually New Low-Calcemic Oxime Analogues of the Hormone 1α,25-Dihydroxyvitamin D3: Synthesis and Biological Testing
Gary H. Posner, Bethany A. Halford, Sara Peleg, Patrick Dolan, and Thomas W. Kensler
pp 1723–1730Publication Date (Web): March 07, 2002 (Article)
DOI: 10.1021/jm010560o
Brief Articles
A Comparative Molecular Field Analysis (COMFA) of the Structural Determinants of Heat-Stable Enterotoxins Mediating Activation of Guanylyl Cyclase C
Henry R. Wolfe and Scott A. Waldman
pp 1731–1734Publication Date (Web): March 13, 2002 (Brief Article)
DOI: 10.1021/jm010208a
Additions and Corrections
Antimalarial Alkoxylated and Hydroxylated Chalcones: Structure−Activity Relationship Analysis.
Mei Liu, Prapon Wilairat, and Mei-Lin Go:
p 1735Publication Date (Web): February 26, 2002 (Addition/Correction)
DOI: 10.1021/jm010572+