Table of Contents
March 27, 2003
Volume 46, Issue 7
Pages 1081-1278
Perspectives
Antiestrogens and Selective Estrogen Receptor Modulators as Multifunctional Medicines. 2. Clinical Considerations and New Agents
V. Craig Jordan
pp 1081–1111Publication Date (Web): February 27, 2003 (Perspective)
DOI: 10.1021/jm020450x
Hi-Res PDFSynthesis and Biological Evaluation of Non-Peptidic Cyclophilin Ligands
Yong-Qian Wu, Sergei Belyakov, Chi Choi, David Limburg, Bert E. Thomas IV, Mark Vaal, Ling Wei, Douglas E. Wilkinson, Agnes Holmes, Mike Fuller, Jocelyn McCormick, Maureen Connolly, Tim Moeller, Joseph Steiner, and Gregory S. Hamilton
pp 1112–1115Publication Date (Web): February 25, 2003 (Letter)
DOI: 10.1021/jm020409u
Discovery of 5-[5-Fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic Acid (2-Diethylaminoethyl)amide, a Novel Tyrosine Kinase Inhibitor Targeting Vascular Endothelial and Platelet-Derived Growth Factor Receptor Tyrosine Kinase
Li Sun, Chris Liang, Sheri Shirazian, Yong Zhou, Todd Miller, Jean Cui, Juri Y. Fukuda, Ji-Yu Chu, Asaad Nematalla, Xueyan Wang, Hui Chen, Anand Sistla, Tony C. Luu, Flora Tang, James Wei, and Cho Tang
pp 1116–1119Publication Date (Web): March 05, 2003 (Letter)
DOI: 10.1021/jm0204183
Pyrrolopyrazinedione-Based Inhibitors of Human Hormone-Sensitive Lipase
Deborah H. Slee, Abhijit S. Bhat, Truc N. Nguyen, Mary Kish, Katy Lundeen, Michael J. Newman, and Stephen J. McConnell
pp 1120–1122Publication Date (Web): February 28, 2003 (Letter)
DOI: 10.1021/jm020460y
Discovery of Tyrosine-Based Potent and Selective Melanocortin-1 Receptor Small-Molecule Agonists with Anti-inflammatory Properties
Timothy F. Herpin, Guixue Yu, Kenneth E. Carlson, George C. Morton, Ximao Wu, Liya Kang, Huji Tuerdi, Ashish Khanna, John S. Tokarski, R. Michael Lawrence, and John E. Macor
pp 1123–1126Publication Date (Web): February 20, 2003 (Letter)
DOI: 10.1021/jm025600i
Design and Synthesis of Naphthalenic Dimers as Selective MT1 Melatoninergic Ligands
Carole Descamps-François, Saïd Yous, Philippe Chavatte, Valérie Audinot, Anne Bonnaud, Jean A. Boutin, Philippe Delagrange, Caroline Bennejean, Pierre Renard, and Daniel Lesieur
pp 1127–1129Publication Date (Web): March 01, 2003 (Letter)
DOI: 10.1021/jm0255872
In Vitro and in Vivo Antitumor Properties of Tetrakis((trishydroxy- methyl)phosphine)gold(I) Chloride
Nagavarakishore Pillarsetty, Kavita K. Katti, Timothy J. Hoffman, Wynn A. Volkert, Kattesh V. Katti, Hideo Kamei, and Tatsurou Koide
pp 1130–1132Publication Date (Web): February 27, 2003 (Letter)
DOI: 10.1021/jm025615g
Articles
Virtual Screening for Submicromolar Leads of tRNA-guanine Transglycosylase Based on a New Unexpected Binding Mode Detected by Crystal Structure Analysis
Ruth Brenk, Lars Naerum, Ulrich Grädler, Hans-Dieter Gerber, George A. Garcia, Klaus Reuter, Milton T. Stubbs, and Gerhard Klebe
pp 1133–1143Publication Date (Web): February 22, 2003 (Article)
DOI: 10.1021/jm0209937
Design, Synthesis, and Pharmacological Profile of Novel Fused Pyrazolo[4,3-d]pyridine and Pyrazolo[3,4-b][1,8]naphthyridine Isosteres: A New Class of Potent and Selective Acetylcholinesterase Inhibitors
Eliezer J. Barreiro, Celso A. Camara, Hugo Verli, Leonora Brazil-Más, Newton G. Castro, Wagner M. Cintra, Yasco Aracava, Carlos R. Rodrigues, and Carlos A. M. Fraga
pp 1144–1152Publication Date (Web): February 28, 2003 (Article)
DOI: 10.1021/jm020391n
Use of a Pharmacophore Model To Discover a New Class of Influenza Endonuclease Inhibitors
Kevin E. B. Parkes, Philipp Ermert, Jürg Fässler, Jane Ives, Joseph A. Martin, John H. Merrett, Daniel Obrecht, Glyn Williams, and Klaus Klumpp
pp 1153–1164Publication Date (Web): February 20, 2003 (Article)
DOI: 10.1021/jm020334u
Synthesis of Novel Thrombin Inhibitors. Use of Ring-Closing Metathesis Reactions for Synthesis of P2 Cyclopentene- and Cyclohexenedicarboxylic Acid Derivatives
Fredrik Thorstensson, Ingemar Kvarnström, Djordje Musil, Ingemar Nilsson, and Bertil Samuelsson
pp 1165–1179Publication Date (Web): March 05, 2003 (Article)
DOI: 10.1021/jm021065a
Modes of Methyleneoxy Bridging and Their Effect on Tetrahydronaphthalene Lignan Cytotoxicity
Robert T. LaLonde, Frank Ramdayal, Anatole Sarko, Koichi Yanai, and Mianji Zhang
pp 1180–1190Publication Date (Web): February 22, 2003 (Article)
DOI: 10.1021/jm020158p
New Active Series of Growth Hormone Secretagogues
Vincent Guerlavais, Damien Boeglin, Delphine Mousseaux, Catherine Oiry, Annie Heitz, Romano Deghenghi, Vittorio Locatelli, Antonio Torsello, Corrado Ghé, Filomena Catapano, Giampiero Muccioli, Jean-Claude Galleyrand, Jean-Alain Fehrentz, and Jean Martinez
pp 1191–1203Publication Date (Web): February 25, 2003 (Article)
DOI: 10.1021/jm020985q
Role of the Glycopeptide Framework in the Antibacterial Activity of Hydrophobic Derivatives of Glycopeptide Antibiotics
Svetlana S. Printsevskaya, Andrey Y. Pavlov, Evgenia N. Olsufyeva, Elena P. Mirchink, and Maria N. Preobrazhenskaya
pp 1204–1209Publication Date (Web): February 15, 2003 (Article)
DOI: 10.1021/jm020320o
New Isomeric Azine-Bridged Dinuclear Platinum(II) Complexes Circumvent Cross-Resistance to Cisplatin
Seiji Komeda, Ganna V. Kalayda, Martin Lutz, Anthony L. Spek, Yasuyuki Yamanaka, Takaji Sato, Masahiko Chikuma, and Jan Reedijk
pp 1210–1219Publication Date (Web): February 26, 2003 (Article)
DOI: 10.1021/jm020004+
Full Text HTMLHigh Affinity Hydroxypiperidine Analogues of 4-(2-Benzhydryloxyethyl)-1-(4-fluorobenzyl)piperidine for the Dopamine Transporter: Stereospecific Interactions in Vitro and in Vivo
Sujit K. Ghorai, Charles Cook, Matthew Davis, Sylesh K. Venkataraman, Clifford George, Patrick M. Beardsley, Maarten E. A. Reith, and Aloke K. Dutta
pp 1220–1228Publication Date (Web): March 04, 2003 (Article)
DOI: 10.1021/jm020275k
Design, Synthesis, and Biological Evaluation of C9- and C2-Substituted Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as New A2A and A3 Adenosine Receptors Antagonists
Pier Giovanni Baraldi, Francesca Fruttarolo, Mojgan Aghazadeh Tabrizi, Delia Preti, Romeo Romagnoli, Hussein El-Kashef, Allan Moorman, Katia Varani, Stefania Gessi, Stefania Merighi, and Pier Andrea Borea
pp 1229–1241Publication Date (Web): February 28, 2003 (Article)
DOI: 10.1021/jm021023m
Synthesis and Activity of Substituted 2-Phenylquinolin-4-amines, Antagonists of Immunostimulatory CpG-Oligodeoxynucleotides
Lucjan Strekowski, Martial Say, Maged Henary, Patricia Ruiz, Lori Manzel, Donald E. Macfarlane, and Andrzej J. Bojarski
pp 1242–1249Publication Date (Web): February 20, 2003 (Article)
DOI: 10.1021/jm020374y
A Comparison of Physiochemical Property Profiles of Development and Marketed Oral Drugs
Mark C. Wenlock, Rupert P. Austin, Patrick Barton, Andrew M. Davis, and Paul D. Leeson
pp 1250–1256Publication Date (Web): March 05, 2003 (Article)
DOI: 10.1021/jm021053p
2-(3-Methyl-3H-diaziren-3-yl)ethyl 1-(1-phenylethyl)-1H-imidazole-5-carboxylate: A Derivative of the Stereoselective General Anesthetic Etomidate for Photolabeling Ligand-Gated Ion Channels
S. Shaukat Husain, Michael R. Ziebell, Dirk Ruesch, Filbert Hong, Enrique Arevalo, Jonathan A. Kosterlitz, Richard W. Olsen, Stuart A. Forman, Jonathan B. Cohen, and Keith W. Miller
pp 1257–1265Publication Date (Web): March 05, 2003 (Article)
DOI: 10.1021/jm020465v
Synthesis, Structure Elucidation, in Vitro Biological Activity, Toxicity, and Caco-2 Cell Permeability of Lipophilic Analogues of α-Conotoxin MII
Joanne T. Blanchfield, Julie L. Dutton, Ronald C. Hogg, Oliver P. Gallagher, David J. Craik, Alun Jones, David J. Adams, Richard J. Lewis, Paul F. Alewood, and Istvan Toth
pp 1266–1272Publication Date (Web): March 04, 2003 (Article)
DOI: 10.1021/jm020426j
Brief Articles
Influence of the 5-HT6 Receptor on Acetylcholine Release in the Cortex: Pharmacological Characterization of 4-(2-Bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a Potent and Selective 5-HT6 Receptor Antagonist
Claus Riemer, Edilio Borroni, Bernard Levet-Trafit, James R. Martin, Sonia Poli, Richard H. P. Porter, and Michael Bös
pp 1273–1276Publication Date (Web): February 25, 2003 (Brief Article)
DOI: 10.1021/jm021085c
Book Reviews
Handbook of Pharmaceutical Salts: Properties, Selection, and Use Edited by P. Heinrich Stahl and Camile G. Wermuth. VHCA, Verlag Helvetica Chimica Acta, Zürich, Switzerland, and Wiley-VCH, Weinheim, Germany. 2002. vix + 374 pp. 17.5 × 24.5 cm. ISBN 3-906390-26-8. $130.00
J. Keith Guillory
p 1277Publication Date (Web): February 21, 2003 (Book Review)
DOI: 10.1021/jm030019n
Drug Design. Cutting Edge Approaches Edited by Darren R. Flower. Royal Society of Chemistry, Cambridge, U.K. 2002. x + 192 pp. 16 × 24 cm. ISBN 0-85404-816-2. £59.50
Roger M. Pinder
pp 1277–1278Publication Date (Web): March 01, 2003 (Book Review)
DOI: 10.1021/jm030023z