Table of Contents
December 5, 2002
Volume 45, Issue 25
Pages 5415-5608
About the Cover: Model of the histone deacetylase inhibitor, 3-(4-benzoyl-1-methyl-1H-2-pyrrole)-N-hydroxy-
Letters
Improving the Oral Efficacy of CNS Drug Candidates: Discovery of Highly Orally Efficacious Piperidinyl Piperidine M2 Muscarinic Receptor Antagonists
Yuguang Wang, Samuel Chackalamannil, Zhiyong Hu, William J. Greenlee, John Clader, Craig D. Boyle, James J. Kaminski, William Billard, Herbert Binch, III, Gordon Crosby, Vilma Ruperto, Ruth A. Duffy, Mary Cohen-Williams, Vicki L. Coffin, Kathleen A. Cox, Diane E. Grotz, and Jean E. Lachowicz
pp 5415–5418Publication Date (Web): November 05, 2002 (Letter)
DOI: 10.1021/jm0255163
Hi-Res PDFDiscovery of 8-Hydroxyadenines as a Novel Type of Interferon Inducer
Kosaku Hirota, Kazunori Kazaoka, Itaru Niimoto, Hiroshi Kumihara, Hironao Sajiki, Yoshiaki Isobe, Haruo Takaku, Masanori Tobe, Haruhisa Ogita, Tetsuhiro Ogino, Shinji Ichii, Ayumu Kurimoto, and Hajime Kawakami
pp 5419–5422Publication Date (Web): November 09, 2002 (Letter)
DOI: 10.1021/jm0203581
Telomerase Inhibition, Telomere Shortening, and Decreased Cell Proliferation by Cell Permeable 2‘-O-Methoxyethyl Oligonucleotides
Zhi Chen, Brett P. Monia, and David R. Corey
pp 5423–5425Publication Date (Web): October 31, 2002 (Letter)
DOI: 10.1021/jm025563v
A Thymidine Phosphorylase-Stable Analogue of BVDU with Significant Antiviral Activity
Sven Guenther, Jan Balzarini, Erik De Clercq, and Vasu Nair
pp 5426–5429Publication Date (Web): November 07, 2002 (Letter)
DOI: 10.1021/jm025569k
Articles
Relationships between Structure and Interaction Kinetics for HIV-1 Protease Inhibitors
Per-Olof Markgren, Wesley Schaal, Markku Hämäläinen, Anders Karlén, Anders Hallberg, Bertil Samuelsson, and U. Helena Danielson
pp 5430–5439Publication Date (Web): October 25, 2002 (Article)
DOI: 10.1021/jm0208370
QSAR Evaluation of the Ch'an Su and Related Bufadienolides against the Colchicine-Resistant Primary Liver Carcinoma Cell Line PLC/PRF/51
Yoshiaki Kamano, Ayano Yamashita, Toshihiko Nogawa, Hiroshi Morita, Koichi Takeya, Hideji Itokawa, Toshiaki Segawa, Ayako Yukita, Kyoko Saito, Mariko Katsuyama, and George R. Pettit
pp 5440–5447Publication Date (Web): November 05, 2002 (Article)
DOI: 10.1021/jm0202066
Antitumor Imidazotetrazines. 40.1 Radiosyntheses of [4-11C-Carbonyl]- and [3-N-11C-Methyl]-8-carbamoyl-3-methylimidazo[5,1-d]-1,2,3,5-tetrazin-4(3H)-one (Temozolomide) for Positron Emission Tomography (PET) Studies
Gavin D. Brown, Sajinder K. Luthra, Cathryn S. Brock, Malcolm F. G. Stevens, Patricia M. Price, and Frank Brady
pp 5448–5457Publication Date (Web): November 05, 2002 (Article)
DOI: 10.1021/jm020921f
Antitumor Imidazotetrazines. 41.1 Conjugation of the Antitumor Agents Mitozolomide and Temozolomide to Peptides and Lexitropsins Bearing DNA Major and Minor Groove-Binding Structural Motifs
Jill Arrowsmith, Sharon A. Jennings, Alan S. Clark, and Malcolm F. G. Stevens
pp 5458–5470Publication Date (Web): November 05, 2002 (Article)
DOI: 10.1021/jm020936d
Design and Synthesis of Dipeptide Nitriles as Reversible and Potent Cathepsin S Inhibitors
Yancey D. Ward, David S. Thomson, Leah L. Frye, Charles L. Cywin, Tina Morwick, Michel J. Emmanuel, Renée Zindell, Daniel McNeil, Younes Bekkali, Marc Girardot, Matt Hrapchak, Molly DeTuri, Kathy Crane, Della White, Susan Pav, Yong Wang, Ming-Hong Hao, Christine A. Grygon, Mark E. Labadia, Dorothy M. Freeman, Walter Davidson, Jerry L. Hopkins, Maryanne L. Brown, and Denice M. Spero
pp 5471–5482Publication Date (Web): October 31, 2002 (Article)
DOI: 10.1021/jm020209i
Structural Studies on Hgr3 Orphan Receptor Ligand Prolactin-Releasing Peptide
Anna Maria D'Ursi, Stefania Albrizio, Armida Di Fenza, Orlando Crescenzi, Alfonso Carotenuto, Delia Picone, Ettore Novellino, and Paolo Rovero
pp 5483–5491Publication Date (Web): November 07, 2002 (Article)
DOI: 10.1021/jm020975p
A New Series of Estrogen Receptor Modulators That Display Selectivity for Estrogen Receptor β
Brad R. Henke, Thomas G. Consler, Ning Go, Ron L. Hale, Dana R. Hohman, Stacey A. Jones, Amy T. Lu, Linda B. Moore, John T. Moore, Lisa A. Orband-Miller, R. Graham Robinett, Jean Shearin, Paul K. Spearing, Eugene L. Stewart, Philip S. Turnbull, Susan L. Weaver, Shawn P. Williams, G. Bruce Wisely, and Millard H. Lambert
pp 5492–5505Publication Date (Web): October 26, 2002 (Article)
DOI: 10.1021/jm020291h
Crystal Structures of Dipeptides Containing the Dmt-Tic Pharmacophore
Sharon D. Bryant, Clifford George, Judith L. Flippen-Anderson, Jeffrey R. Deschamps, Severo Salvadori, Gianfranco Balboni, Remo Guerrini, and Lawrence H. Lazarus
pp 5506–5513Publication Date (Web): October 31, 2002 (Article)
DOI: 10.1021/jm020330p
Comparative Molecular Field Analysis of Substrates for an Aryl Sulfotransferase Based on Catalytic Mechanism and Protein Homology Modeling
Vyas Sharma and Michael W. Duffel
pp 5514–5522Publication Date (Web): November 09, 2002 (Article)
DOI: 10.1021/jm010481c
Probing the Cysteine-34 Position of Endogenous Serum Albumin with Thiol-Binding Doxorubicin Derivatives. Improved Efficacy of an Acid-Sensitive Doxorubicin Derivative with Specific Albumin-Binding Properties Compared to That of the Parent Compound
Felix Kratz, André Warnecke, Karin Scheuermann, Cornelia Stockmar, Jürgen Schwab, Peter Lazar, Peter Drückes, Norbert Esser, Joachim Drevs, Didier Rognan, Caterina Bissantz, Caterina Hinderling, Gerd Folkers, Iduna Fichtner, and Clemens Unger
pp 5523–5533Publication Date (Web): November 09, 2002 (Article)
DOI: 10.1021/jm020276c
Perfluorooctyl Bromide Has Limited Membrane Solubility and Is Located at the Bilayer Center. Locating Small Molecules in Lipid Bilayers through Paramagnetic Enhancements of NMR Relaxation
Jeffrey F. Ellena, Viktor V. Obraztsov, Valerie L. Cumbea, Catherine M. Woods, and David S. Cafiso
pp 5534–5542Publication Date (Web): November 07, 2002 (Article)
DOI: 10.1021/jm020278x
Pyrimidoquinazoline-Based Antitumor Agents. Design of Topoisomerase II to DNA Cross-linkers with Activity against Protein Kinases
Edward B. Skibo, Xiaofen Huang, Rogelio Martinez, Robert H. Lemus, and William A. CraigoRobert T. Dorr
pp 5543–5555Publication Date (Web): November 05, 2002 (Article)
DOI: 10.1021/jm020285l
Potent δ-Opioid Receptor Agonists Containing the Dmt−Tic Pharmacophore
Gianfranco Balboni, Severo Salvadori, Remo Guerrini, Lucia Negri, Elisa Giannini, Yunden Jinsmaa, Sharon D. Bryant, and Lawrence H. Lazarus
pp 5556–5563Publication Date (Web): November 09, 2002 (Article)
DOI: 10.1021/jm020336e
Synthesis and Structure−Activity Relationships of Novel 7-Substituted 1,4-Dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic Acids as Antitumor Agents. Part 1
Kyoji Tomita, Yasunori Tsuzuki, Koh-ichiro Shibamori, Masanori Tashima, Fumie Kajikawa, Yuji Sato, Shigeki Kashimoto, Katsumi Chiba, and Katsuhiko Hino
pp 5564–5575Publication Date (Web): November 01, 2002 (Article)
DOI: 10.1021/jm010057b
Use of ab Initio Calculations To Predict the Biological Potency of Carboxylesterase Inhibitors
Craig E. Wheelock, Michael E. Colvin, Ippei Uemura, Marilyn M. Olmstead, James R. Sanborn, Yoshiaki Nakagawa, A. Daniel Jones, and Bruce D. Hammock
pp 5576–5593Publication Date (Web): November 07, 2002 (Article)
DOI: 10.1021/jm020072w
Syntheses and Structure−Activity Relationships of Nonnatural β-C-Nucleoside 5‘-Triphosphates Bearing an Aromatic Nucleobase with Phenolic Hydroxy Groups: Inhibitory Activities against DNA Polymerases
Saeko Aketani, Kentaro Tanaka, Kaneyoshi Yamamoto, Akira Ishihama, Honghua Cao, Atsushi Tengeiji, Shuichi Hiraoka, Motoo Shiro, and Mitsuhiko Shionoya
pp 5594–5603Publication Date (Web): November 09, 2002 (Article)
DOI: 10.1021/jm020193w
Brief Articles
Synthesis and Antimycobacterial Activity of Pyrazine and Quinoxaline Derivatives
Lainne E. Seitz, William J. Suling, and Robert C. Reynolds
pp 5604–5606Publication Date (Web): November 07, 2002 (Brief Article)
DOI: 10.1021/jm020310n
Book Reviews
Enzymes. A Practical Introduction to Structure, Mechanism, and Data Analysis. Second Edition By Robert A. Copeland. Wiley-VCH, New York. 2000. xvi + 397 pp. 16 × 24.5 cm. ISBN 0-471-35929-7. $99.95.
D. Eric Walters
p 5607Publication Date (Web): November 09, 2002 (Book Review)
DOI: 10.1021/jm020467f
Additions and Corrections
Structural Basis for Understanding Structure−Activity Relationships for the Glutamate Binding Site of the NMDA Receptor.
Irina G. Tikhonova, Igor I. Baskin, Vladimir A. Palyulin, Nikolai S. Zefirov, and Sergey O. Bachurin:
p 5608Publication Date (Web): November 06, 2002 (Addition/Correction)
DOI: 10.1021/jm021040b