Table of Contents
February 13, 2003
Volume 46, Issue 4
Pages 445-653
Perspectives
Ernest Guenther Award in Chemistry of Natural Products. Amphibian Skin: A Remarkable Source of Biologically Active Arthropod Alkaloids
John W. Daly
pp 445–452Publication Date (Web): December 31, 2002 (Perspective)
DOI: 10.1021/jm0204845
Hi-Res PDFDesign and Synthesis of 8-Hydroxy-[1,6]Naphthyridines as Novel Inhibitors of HIV-1 Integrase in Vitro and in Infected Cells
Linghang Zhuang, John S. Wai, Mark W. Embrey, Thorsten E. Fisher, Melissa S. Egbertson, Linda S. Payne, James P. Guare, Jr., Joseph P. Vacca, Daria J. Hazuda, Peter J. Felock, Abigail L. Wolfe, Kara A. Stillmock, Marc V. Witmer, Gregory Moyer, William A. Schleif, Lori J. Gabryelski, Yvonne M. Leonard, Joseph J. Lynch, Jr., Stuart R. Michelson, and Steven D. Young
pp 453–456Publication Date (Web): January 09, 2003 (Letter)
DOI: 10.1021/jm025553u
Substituted Pyrazolopyridopyridazines as Orally Bioavailable Potent and Selective PDE5 Inhibitors: Potential Agents for Treatment of Erectile Dysfunction
Guixue Yu, Helen Mason, Ximao Wu, Jian Wang, Saeho Chong, Bruce Beyer, Andrew Henwood, Ronald Pongrac, Laurie Seliger, Bin He, Diane Normandin, Pam Ferrer, Rongan Zhang, Leonard Adam, William G. Humphrey, John Krupinski, and John E. Macor
pp 457–460Publication Date (Web): January 08, 2003 (Letter)
DOI: 10.1021/jm0256068
Articles
Metabolism-Directed Optimization of 3-Aminopyrazinone Acetamide Thrombin Inhibitors. Development of an Orally Bioavailable Series Containing P1 and P3 Pyridines
Christopher S. Burgey, Kyle A. Robinson, Terry A. Lyle, Philip E. J. Sanderson, S. Dale Lewis, Bobby J. Lucas, Julie A. Krueger, Rominder Singh, Cynthia Miller-Stein, Rebecca B. White, Bradley Wong, Elizabeth A. Lyle, Peter D. Williams, Craig A. Coburn, Bruce D. Dorsey, James C. Barrow, Maria T. Stranieri, Marie A. Holahan, Gary R. Sitko, Jacquelynn J. Cook, Daniel R. McMasters, Colleen M. McDonough, William M. Sanders, Audrey A. Wallace, Franklin C. Clayton, Dennis Bohn, Yvonne M. Leonard, Theodore J. Detwiler, Jr., Joseph J. Lynch, Jr., Youwei Yan, Zhongguo Chen, Lawrence Kuo, Stephen J. Gardell, Jules A. Shafer, and Joseph P. Vacca
pp 461–473Publication Date (Web): January 08, 2003 (Article)
DOI: 10.1021/jm020311f
Structure-Based de Novo Design, Synthesis, and Biological Evaluation of Non-Azole Inhibitors Specific for Lanosterol 14α-Demethylase of Fungi
Haitao Ji, Wannian Zhang, Min Zhang, Makiko Kudo, Yuri Aoyama, Yuzo Yoshida, Chunquan Sheng, Yunlong Song, Song Yang, Youjun Zhou, Jiaguo Lü, and Jü Zhu
pp 474–485Publication Date (Web): January 18, 2003 (Article)
DOI: 10.1021/jm020362c
Identification, Synthesis, and Activity of Novel Blockers of the Voltage-Gated Potassium Channel Kv1.5
Stefan Peukert, Joachim Brendel, Bernard Pirard, Andrea Brüggemann, Peter Below, Heinz-Werner Kleemann, Horst Hemmerle, and Wolfgang Schmidt
pp 486–498Publication Date (Web): January 21, 2003 (Article)
DOI: 10.1021/jm0210461
Surflex: Fully Automatic Flexible Molecular Docking Using a Molecular Similarity-Based Search Engine
Ajay N. Jain
pp 499–511Publication Date (Web): January 21, 2003 (Article)
DOI: 10.1021/jm020406h
3-(4-Aroyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-alkylamides as a New Class of Synthetic Histone Deacetylase Inhibitors. 1. Design, Synthesis, Biological Evaluation, and Binding Mode Studies Performed through Three Different Docking Procedures
Antonello Mai, Silvio Massa, Rino Ragno, Ilaria Cerbara, Florian Jesacher, Peter Loidl, and Gerald Brosch
pp 512–524Publication Date (Web): January 21, 2003 (Article)
DOI: 10.1021/jm021070e
Antineoplastic Agents. 487. Synthesis and Biological Evaluation of the Antineoplastic Agent 3,4-Methylenedioxy-5,4‘-dimethoxy-3‘-amino-Z-stilbene and Derived Amino Acid Amides
George R. Pettit, Collin R. Anderson, Delbert L. Herald, M. Katherine Jung, Debbie J. Lee, Ernest Hamel, and Robin K. Pettit
pp 525–531Publication Date (Web): January 10, 2003 (Article)
DOI: 10.1021/jm020204l
4-Substituted 4-Hydroxycyclohexa-2,5-dien-1-ones with Selective Activities against Colon and Renal Cancer Cell Lines
Geoffrey Wells, Jane M. Berry, Tracey D. Bradshaw, Angelika M. Burger, Angela Seaton, Bo Wang, Andrew D. Westwell, and Malcolm F. G. Stevens
pp 532–541Publication Date (Web): January 21, 2003 (Article)
DOI: 10.1021/jm020984y
Synthesis and in Vitro and in Vivo Antimalarial Activity of N1-(7-Chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine Derivatives
Adina Ryckebusch, Rébecca Deprez-Poulain, Louis Maes, Marie-Ange Debreu-Fontaine, Elisabeth Mouray, Philippe Grellier, and Christian Sergheraert
pp 542–557Publication Date (Web): January 21, 2003 (Article)
DOI: 10.1021/jm020960r
Absorption Classification of Oral Drugs Based on Molecular Surface Properties
Christel A. S. Bergström, Melissa Strafford, Lucia Lazorova, Alex Avdeef, Kristina Luthman, and Per Artursson
pp 558–570Publication Date (Web): January 11, 2003 (Article)
DOI: 10.1021/jm020986i
Design, Synthesis, and Biological Evaluation of a Series of Fluoroquinoanthroxazines with Contrasting Dual Mechanisms of Action against Topoisomerase II and G-Quadruplexes
Mu-Yong Kim, Wenhu Duan, Mary Gleason-Guzman, and Laurence H. Hurley
pp 571–583Publication Date (Web): January 04, 2003 (Article)
DOI: 10.1021/jm0203377
Orally Active Analogues of the Dopaminergic Prodrug 6-(N,N-Di-n-propylamino)-3,4,5,6,7,8-hexahydro-2H-naphthalen-1-one: Synthesis and Pharmacological Activity
Bastiaan J. Venhuis, Durk Dijkstra, David J. Wustrow, Leonard T. Meltzer, Lawrence D. Wise, Stephen J. Johnson, Thomas G. Heffner, and Håkan V. Wikström
pp 584–590Publication Date (Web): January 09, 2003 (Article)
DOI: 10.1021/jm020990u
Design, Synthesis, and Biological Activities of Classical N-{4-[2-(2-Amino-4-ethylpyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-l-glutamic Acid and Its 6-Methyl Derivative as Potential Dual Inhibitors of Thymidylate Synthase and Dihydrofolate Reductase and as Potential Antitumor Agents1
Aleem Gangjee, Jianming Yu, Roy L. Kisliuk, William H. Haile, Giulia Sobrero, and John J. McGuire
pp 591–600Publication Date (Web): January 21, 2003 (Article)
DOI: 10.1021/jm0203534
Preparation of 7-Substituted Ginkgolide Derivatives: Potent Platelet Activating Factor (PAF) Receptor Antagonists
Stine Byskov Vogensen, Kristian Strømgaard, Hideo Shindou, Stanislav Jaracz, Makiko Suehiro, Satoshi Ishii, Takao Shimizu, and Koji Nakanishi
pp 601–608Publication Date (Web): January 21, 2003 (Article)
DOI: 10.1021/jm0203985
Syntheses and Antiproliferative Activities of 7-Azarebeccamycin Analogues Bearing One 7-Azaindole Moiety
Christelle Marminon, Alain Pierré, Bruno Pfeiffer, Valérie Pérez, Stéphane Léonce, Alexandra Joubert, Christian Bailly, Pierre Renard, John Hickman, and Michelle Prudhomme
pp 609–622Publication Date (Web): January 18, 2003 (Article)
DOI: 10.1021/jm0210055
3-(αR)-α-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)- N-alkyl-N-arylbenzamides: Potent, Non-Peptidic Agonists of Both the μ and δ Opioid Receptors
Michael J. Bishop, Dulce M. Garrido, G. Evan Boswell, Mark A. Collins, Philip A. Harris, Robert W. McNutt, Scott J. O'Neill, Ke Wei, and Kwen-Jen Chang
pp 623–633Publication Date (Web): January 21, 2003 (Article)
DOI: 10.1021/jm020395s
Brief Articles
CC-1065 Analogues Bearing Different DNA-Binding Subunits: Synthesis, Antitumor Activity, and Preliminary Toxicity Study
Yuqiang Wang, Lianfa Li, Wenqing Ye, Zhiming Tian, Wei Jiang, Hong Wang, Susan C. Wright, and James W. Larrick
pp 634–637Publication Date (Web): January 11, 2003 (Brief Article)
DOI: 10.1021/jm0203433
New Semisynthetic Quassinoids with in Vivo Antimalarial Activity
Nobutoshi Murakami, Masanori Sugimoto, Motoyuki Kawanishi, Satoru Tamura, Hye-Sook Kim, Khurshida Begum, Yusuke Wataya, and Motomasa Kobayashi
pp 638–641Publication Date (Web): January 18, 2003 (Brief Article)
DOI: 10.1021/jm0201971
Synthesis, Structure−Activity Relationship, and Evaluation of SR141716 Analogues: Development of Central Cannabinoid Receptor Ligands with Lower Lipophilicity
Reeti Katoch-Rouse, Olga A. Pavlova, Tara Caulder, Alexander F. Hoffman, Alexey G. Mukhin, and Andrew G. Horti
pp 642–645Publication Date (Web): January 18, 2003 (Brief Article)
DOI: 10.1021/jm020157x
Synthesis and Structure−Affinity Relationships of 1-[ω-(4-Aryl-1-piperazinyl)alkyl]-1-aryl Ketones as 5-HT7 Receptor Ligands
Roberto Perrone, Francesco Berardi, Nicola A. Colabufo, Enza Lacivita, Marcello Leopoldo, and Vincenzo Tortorella
pp 646–649Publication Date (Web): January 18, 2003 (Brief Article)
DOI: 10.1021/jm020994z
Book Reviews
New Drugs 2001. Including All Drugs Approved in 2000 and 2001 Edited by G. W. A. Milne. Ashgate Publishing Company, Burlington, VT. 2002. xxiii + 154 pp. 12.5 × 25 cm. ISBN 0-566-08516-X. $90.00.
Carl Kaiser
p 650Publication Date (Web): January 10, 2003 (Book Review)
DOI: 10.1021/jm0204744
Scientists Must Speak By D. Eric Walters and Gale Climenson Walters. Routledge, London and New York. 2002. xii + 132 pp. 14 × 21.5 cm. ISBN 0-415-28028-1. $18.95 (paperback).
John R. J. Sorenson
p 650Publication Date (Web): January 11, 2003 (Book Review)
DOI: 10.1021/jm020552n
p 651
Publication Date (Web): January 17, 2003 (Book Review)
DOI: 10.1021/jm020553f
Additions and Corrections
Structure−Activity Studies on Anticonvulsant Sugar Sulfamates Related to Topiramate. Enhanced Potency with Cyclic Sulfate Derivatives.
Bruce E. Maryanoff, Michael J. Costanzo, Samuel O. Nortey, Michael N. Greco, Richard P. Shank, James J. Schupsky, Marta P. Ortegon, and Jeffry L. Vaught:
p 652Publication Date (Web): January 18, 2003 (Addition/Correction)
DOI: 10.1021/jm020527h
New Approach to Pharmacophore Mapping and QSAR Analysis Using Inductive Logic Programming. Application to Thermolysin Inhibitors and Glycogen Phosphorylase b Inhibitors
Nathalie Marchand-Geneste, Kimberly A. Watson, Bjørn K Alsberg, and Ross D. King:
p 653Publication Date (Web): January 15, 2003 (Addition/Correction)
DOI: 10.1021/jm020948z