Table of Contents
December 4, 2003
Volume 46, Issue 25
Pages 5277-5552
About the Cover: Connolly surface map of the X-ray structure of the α-thrombin-cyclopentenedicarboxylic acid derivative complex (yellow) at 1.9 Å resolution superimposed on the X-ray structure of the α-thrombin-PPACK complex (magenta) (Thorstensson, F.; et al. J. Med. Chem. 2003, 46, 1165-1179).
Perspective
Molecular Basis of Neurotrophin−Receptor Interactions
Mookda Pattarawarapan and Kevin Burgess
pp 5277–5291Publication Date (Web): November 14, 2003 (Perspective)
DOI: 10.1021/jm030221q
Hi-Res PDF Letters
Design, Synthesis, and Biological Activity of a Difluoro-Substituted, Conformationally Rigid Vigabatrin Analogue as a Potent γ-Aminobutyric Acid Aminotransferase Inhibitor
Yue Pan, Jian Qiu, and Richard B. Silverman
pp 5292–5293Publication Date (Web): November 11, 2003 (Letter)
DOI: 10.1021/jm034162s
Synthesis and Evaluation of Imidazole Acetic Acid Inhibitors of Activated Thrombin-Activatable Fibrinolysis Inhibitor as Novel Antithrombotics
James C. Barrow, Philippe G. Nantermet, Shaun R. Stauffer, Phung L. Ngo, Melissa A. Steinbeiser, Shi-Shan Mao, Steven S. Carroll, Carolyn Bailey, Dennis Colussi, Michelle Bosserman, Christine Burlein, Jacquelynn J. Cook, Gary Sitko, Philip R. Tiller, Cynthia M. Miller-Stein, Mark Rose, Daniel R. McMasters, Joseph P. Vacca, and Harold G. Selnick
pp 5294–5297Publication Date (Web): November 01, 2003 (Letter)
DOI: 10.1021/jm034141y
Articles
Discovery of 1-(2-Aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2‘-(aminosulfonyl)[1,1‘-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a Potent, Selective, and Orally Bioavailable Factor Xa Inhibitor1
James R. Pruitt, Donald J. P. Pinto, Robert A. Galemmo, Jr., Richard S. Alexander, Karen A. Rossi, Brian L. Wells, Spencer Drummond, Lori L. Bostrom, Debra Burdick, Robert Bruckner, Haiying Chen, Angela Smallwood, Pancras C. Wong, Matthew R. Wright, Steven Bai, Joseph M. Luettgen, Robert M. Knabb, Patrick Y. S. Lam, and Ruth R. Wexler
pp 5298–5315Publication Date (Web): October 29, 2003 (Article)
DOI: 10.1021/jm030212h
Molecular Model of the αIIbβ3 Integrin
Bradley P. Feuston, J. Christopher Culberson, and George D. Hartman
pp 5316–5325Publication Date (Web): October 30, 2003 (Article)
DOI: 10.1021/jm030146j
A Method for Designing Conformationally Restricted Analogues Based on Allylic Strain: Synthesis of a Novel Class of Noncompetitive NMDA Receptor Antagonists Having the Acrylamide Structure
Yutaka Ohmori, Akitake Yamashita, Ryuichi Tsujita, Tamotsu Yamamoto, Kaku Taniuchi, Akira Matsuda, and Satoshi Shuto
pp 5326–5333Publication Date (Web): October 31, 2003 (Article)
DOI: 10.1021/jm030226n
Neurosteroid Analogues. 9. Conformationally Constrained Pregnanes: Structure−Activity Studies of 13,24-Cyclo-18,21-dinorcholane Analogues of the GABA Modulatory and Anesthetic Steroids (3α,5α)- and (3α,5β)-3-Hydroxypregnan-20-one
Xin Jiang, Brad D. Manion, Ann Benz, Nigam P. Rath, Alex S. Evers, Charles F. Zorumski, Steven Mennerick, and Douglas F. Covey
pp 5334–5348Publication Date (Web): October 30, 2003 (Article)
DOI: 10.1021/jm030302m
Synthesis, Comparative Photosensitizing Efficacy, Human Serum Albumin (Site II) Binding Ability, and Intracellular Localization Characteristics of Novel Benzobacteriochlorins Derived from vic-Dihydroxybacteriochlorins
Guolin Li, Andrew Graham, Yihui Chen, Mahabeer P. Dobhal, Janet Morgan, Gang Zheng, Andrei Kozyrev, Allan Oseroff, Thomas J. Dougherty, and Ravindra K. Pandey
pp 5349–5359Publication Date (Web): November 01, 2003 (Article)
DOI: 10.1021/jm030341y
Application of the λ-Dynamics Method To Evaluate the Relative Binding Free Energies of Inhibitors to HCV Protease
Zhuyan Guo, James Durkin, Thierry Fischmann, Richard Ingram, Andrew Prongay, Rumin Zhang, and Vincent Madison
pp 5360–5364Publication Date (Web): November 11, 2003 (Article)
DOI: 10.1021/jm030040o
Characterization of the 5-HT7 Receptor. Determination of the Pharmacophore for 5-HT7 Receptor Agonism and CoMFA-Based Modeling of the Agonist Binding Site
Erik S. Vermeulen, Anne W. Schmidt, Jeffrey S. Sprouse, Håkan V. Wikström, and Cor J. Grol
pp 5365–5374Publication Date (Web): November 05, 2003 (Article)
DOI: 10.1021/jm030826m
A New Class of Potent Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitors: Structure−Activity Relationships for a Series of 9-Alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the Identification of CEP-5214 and Its Dimethylglycine Ester Prodrug Clinical Candidate CEP-7055
Diane E. Gingrich, Dandu R. Reddy, Mohamed A. Iqbal, Jasbir Singh, Lisa D. Aimone, Thelma S. Angeles, Mark Albom, Shi Yang, Mark A. Ator, Sheryl L. Meyer, Candy Robinson, Bruce A. Ruggeri, Craig A. Dionne, Jeffry L. Vaught, John P. Mallamo, and Robert L. Hudkins
pp 5375–5388Publication Date (Web): October 31, 2003 (Article)
DOI: 10.1021/jm0301641
An Alpha Helix Conformationally Restricted Peptide Is Recognized by Cervical Carcinoma Patients' Sera
Julio C. Calvo, Katia C. Choconta, Diana Diaz, Oscar Orozco, Maria M. Bravo, Fabiola Espejo, Luz M. Salazar, Fanny Guzman, and Manuel E. Patarroyo
pp 5389–5394Publication Date (Web): November 11, 2003 (Article)
DOI: 10.1021/jm030210x
Anticancer Activity of Phenolic Acids of Natural or Synthetic Origin: A Structure−Activity Study
Catarina A. Gomes, Teresa Girão da Cruz, José L. Andrade, Nuno Milhazes, Fernanda Borges, and M. Paula M. Marques
pp 5395–5401Publication Date (Web): November 11, 2003 (Article)
DOI: 10.1021/jm030956v
New Lupane Derived Compounds with Pro-Apoptotic Activity in Cancer Cells: Synthesis and Structure−Activity Relationships
Jan Šarek, Jiří Klinot, Petr Džubák, Eva Klinotová, Věra Nosková, Václav Křeček, Gabriela Kořínková, Jean Oliver Thomson, Anna Janošt'áková, Shudong Wang, Simon Parsons, Peter M. Fischer, Nikolai Z. Zhelev, and Marián Hajdúch
pp 5402–5415Publication Date (Web): November 12, 2003 (Article)
DOI: 10.1021/jm020854p
Pyrazole and Isoxazole Derivatives as New, Potent, and Selective 20-Hydroxy-5,8,11,14-eicosatetraenoic Acid Synthase Inhibitors
Toshio Nakamura, Masakazu Sato, Hiroyuki Kakinuma, Noriyuki Miyata, Kazuo Taniguchi, Kagumi Bando, Ayumi Koda, and Kazuya Kameo
pp 5416–5427Publication Date (Web): November 11, 2003 (Article)
DOI: 10.1021/jm020557k
1,2-Benzisoxazole Phosphorodiamidates as Novel Anticancer Prodrugs Requiring Bioreductive Activation
Monish Jain and Chul-Hoon Kwon
pp 5428–5436Publication Date (Web): November 12, 2003 (Article)
DOI: 10.1021/jm020581y
Synthesis and Biological Evaluation of 4-Arylcoumarin Analogues of Combretastatins
Christian Bailly, Christine Bal, Pascale Barbier, Sébastien Combes, Jean-Pierre Finet, Marie-Paule Hildebrand, Vincent Peyrot, and Nicole Wattez
pp 5437–5444Publication Date (Web): October 31, 2003 (Article)
DOI: 10.1021/jm030903d
Synthesis and Structure−Activity Relationships of Conformationally Constrained Histamine H3 Receptor Agonists
Ruengwit Kitbunnadaj, Obbe P. Zuiderveld, Iwan J. P. De Esch, Roeland C. Vollinga, Remko Bakker, Martin Lutz, Anthony L. Spek, Emile Cavoy, Marie-France Deltent, Wiro M. P. B. Menge, Henk Timmerman, and Rob Leurs
pp 5445–5457Publication Date (Web): November 01, 2003 (Article)
DOI: 10.1021/jm030905y
Nα-Imidazolylalkyl and Pyridylalkyl Derivatives of Histaprodifen: Synthesis and in Vitro Evaluation of Highly Potent Histamine H1-Receptor Agonists
Sonja Menghin, Heinz H. Pertz, Kai Kramer, Roland Seifert, Walter Schunack, and Sigurd Elz
pp 5458–5470Publication Date (Web): October 31, 2003 (Article)
DOI: 10.1021/jm0309147
Carbonic Anhydrase Inhibitors: Inhibition of Transmembrane, Tumor-Associated Isozyme IX, and Cytosolic Isozymes I and II with Aliphatic Sulfamates
Jean-Yves Winum, Daniela Vullo, Angela Casini, Jean-Louis Montero, Andrea Scozzafava, and Claudiu T. Supuran
pp 5471–5477Publication Date (Web): November 07, 2003 (Article)
DOI: 10.1021/jm030911u
Polyamine−Iron Chelator Conjugate
Raymond J. Bergeron, James S. McManis, April M. Franklin, Hua Yao, and William R. Weimar
pp 5478–5483Publication Date (Web): November 11, 2003 (Article)
DOI: 10.1021/jm0302694
Synthesis and Structure−Activity Relationship of Novel, Highly Potent Metharyl and Methcycloalkyl Cyclooxygenase-2 (COX-2) Selective Inhibitors
Subhash P. Khanapure, David S. Garvey, Delano V. Young, Maiko Ezawa, Richard A. Earl, Rick D. Gaston, Xinqin Fang, Madhavi Murty, Allison Martino, Matthew Shumway, Mark Trocha, Przemyslaw Marek, S. William Tam, David R. Janero, and L. Gordon Letts
pp 5484–5504Publication Date (Web): November 07, 2003 (Article)
DOI: 10.1021/jm030268b
Guanidino N-Substituted and N,N-Disubstituted Derivatives of the κ-Opioid Antagonist GNTI
Shannon L. Black, Cedric Chauvignac, Peter Grundt, Carl N. Miller, Susan Wood, John R. Traynor, John W. Lewis, and Stephen M. Husbands
pp 5505–5511Publication Date (Web): November 12, 2003 (Article)
DOI: 10.1021/jm0309203
Syntheses and Binding Studies of New [(Aryl)(aryloxy)methyl]piperidine Derivatives and Related Compounds as Potential Antidepressant Drugs with High Affinity for Serotonin (5-HT) and Norepinephrine (NE) Transporters
Aurelio Orjales, Ramón Mosquera, Antonio Toledo, M. Carmen Pumar, Neftalí García, Lourdes Cortizo, Luis Labeaga, and Ana Innerárity
pp 5512–5532Publication Date (Web): November 01, 2003 (Article)
DOI: 10.1021/jm0309349
Synthesis and Evaluation of Nitroheterocyclic Carbamate Prodrugs for Use with Nitroreductase-Mediated Gene-Directed Enzyme Prodrug Therapy
Michael P. Hay, Robert F. Anderson, Dianne M. Ferry, William R. Wilson, and William A. Denny
pp 5533–5545Publication Date (Web): October 31, 2003 (Article)
DOI: 10.1021/jm030308b
Synthesis of a Prodrug Designed To Release Multiple Inhibitors of the Epidermal Growth Factor Receptor Tyrosine Kinase and an Alkylating Agent: A Novel Tumor Targeting Concept
Ranjita Banerjee, Zakaria Rachid, James McNamee, and Bertrand J. Jean-Claude
pp 5546–5551Publication Date (Web): November 07, 2003 (Article)
DOI: 10.1021/jm030423m
Book Reviews
Analgesics. From Chemistry and Pharmacology to Clinical Application Edited by H. Buschmann, T. Christoph, E. Friderichs, C. Maul, and B. Sundermann. Wiley-VCH, Weinheim, Germany. 2002. ix + 604 pp. 18 × 25 cm. ISBN 3527304037. $185.00.
David S. Fries
p 5552Publication Date (Web): November 11, 2003 (Book Review)
DOI: 10.1021/jm030187f