Table of Contents
February 14, 2002
Volume 45, Issue 4
Pages 753-994
Letters
Inhibitors of Human Histone Deacetylase: Synthesis and Enzyme and Cellular Activity of Straight Chain Hydroxamates
Stacy W. Remiszewski, Lidia C. Sambucetti, Peter Atadja, Kenneth W. Bair, Wendy D. Cornell, Michael A. Green, Kobporn Lulu Howell, Manfred Jung, Paul Kwon, Nancy Trogani, and Heather Walker
pp 753–757Publication Date (Web): January 17, 2002 (Letter)
DOI: 10.1021/jm015568c
Hi-Res PDFDNA Cleavage Potency, Cytotoxicity, and Mechanism of Action of a Novel Class of Enediyne Prodrugs
Wei-Min Dai, Kwong Wah Lai, Anxin Wu, Wataru Hamaguchi, Mavis Yuk Ha Lee, Ling Zhou, Atsushi Ishii, and Sei-ichi Nishimoto
pp 758–761Publication Date (Web): January 17, 2002 (Letter)
DOI: 10.1021/jm015588e
Articles
Environmental Mimic of Receptor Interaction: Conformational Analysis of CCK-15 in Solution
Stefania Albrizio, Alfonso Carotenuto, Caterina Fattorusso, Luis Moroder, Delia Picone, Piero A. Temussi, and Annamaria D'Ursi
pp 762–769Publication Date (Web): January 22, 2002 (Article)
DOI: 10.1021/jm0109457
Synthesis, Biological Activity, and Molecular Modeling Investigation of New Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine Derivatives as Human A3 Adenosine Receptor Antagonists
Pier Giovanni Baraldi, Barbara Cacciari, Stefano Moro, Giampiero Spalluto, Giorgia Pastorin, Tatiana Da Ros, Karl-Norbert Klotz, Katia Varani, Stefania Gessi, and Pier Andrea Borea
pp 770–780Publication Date (Web): January 11, 2002 (Article)
DOI: 10.1021/jm0109614
A Three-Dimensional Quantitative Structure−Activity Relationship Study of Heparin-Binding Epidermal Growth Factor Shedding Inhibitors Using Comparative Molecular Field Analysis
Roberta Bursi, Masaaki Sawa, Yasuyuki Hiramatsu, and Hirosato Kondo
pp 781–788Publication Date (Web): January 18, 2002 (Article)
DOI: 10.1021/jm0110385
Novel Tricyclic-α-alkyloxyphenylpropionic Acids: Dual PPARα/γ Agonists with Hypolipidemic and Antidiabetic Activity
Per Sauerberg, Ingrid Pettersson, Lone Jeppesen, Paul S. Bury, John P. Mogensen, Karsten Wassermann, Christian L. Brand, Jeppe Sturis, Helle F. Wöldike, Jan Fleckner, Anne-Sofie T. Andersen, Steen B. Mortensen, L. Anders Svensson, Hanne B. Rasmussen, Søren V. Lehmann, Zdenek Polivka, Karel Sindelar, Vladimira Panajotova, Lars Ynddal, and Erik M. Wulff
pp 789–804Publication Date (Web): January 23, 2002 (Article)
DOI: 10.1021/jm010964g
Minor Groove DNA Binders as Antimicrobial Agents. 1. Pyrrole Tetraamides Are Potent Antibacterials against Vancomycin Resistant Enteroccoci and Methicillin Resistant Staphylococcus aureus
Natalia B. Dyatkina, Christopher D. Roberts, Jesse D. Keicher, Yuqin Dai, Joshua P. Nadherny, Wentao Zhang, Uli Schmitz, Ana Kongpachith, Kevin Fung, Alexander A. Novikov, Lillian Lou, Mark Velligan, Alexander A. Khorlin, and Ming S. Chen
pp 805–817Publication Date (Web): January 11, 2002 (Article)
DOI: 10.1021/jm010375a
Mining the National Cancer Institute's Tumor-Screening Database: Identification of Compounds with Similar Cellular Activities
Alfred A. Rabow, Robert H. Shoemaker, Edward A. Sausville, and David G. Covell
pp 818–840Publication Date (Web): January 23, 2002 (Article)
DOI: 10.1021/jm010385b
CoMFA and CoMSIA 3D QSAR and Docking Studies on Conformationally-Restrained Cinnamoyl HIV-1 Integrase Inhibitors: Exploration of a Binding Mode at the Active Site
John K. Buolamwini and Haregewein Assefa
pp 841–852Publication Date (Web): January 22, 2002 (Article)
DOI: 10.1021/jm010399h
Structural Basis of RasGRP Binding to High-Affinity PKC Ligands
Suo-Bao Rong, Istvan J. Enyedy, Lixin Qiao, Lianyun Zhao, Dawei Ma, Larry L. Pearce, Patricia S. Lorenzo, James C. Stone, Peter M. Blumberg, Shaomeng Wang, and Alan P. Kozikowski
pp 853–860Publication Date (Web): January 22, 2002 (Article)
DOI: 10.1021/jm010422z
DNA Cross-Linking by Azinomycin B: Monte Carlo Simulations in the Evaluation of Sequence Selectivity
Stefano Alcaro, Francesco Ortuso, and Robert S. Coleman
pp 861–870Publication Date (Web): January 10, 2002 (Article)
DOI: 10.1021/jm011040w
A 3·(ET743)-DNA Complex That Both Resembles an RNA-DNA Hybrid and Mimicks Zinc Finger-Induced DNA Structural Distortions
Esther Marco, Raquel García-Nieto, Jesús Mendieta, Ignacio Manzanares, Carmen Cuevas, and Federico Gago
pp 871–880Publication Date (Web): January 19, 2002 (Article)
DOI: 10.1021/jm010370d
Designing Analogues of Mini Atrial Natriuretic Peptide Based on Structural Analysis by NMR and Restrained Molecular Dynamics
Kenji Sugase, Yoshiaki Oyama, Katsuhiko Kitano, Takashi Iwashita, Toshimichi Fujiwara, Hideo Akutsu, and Masaji Ishiguro
pp 881–887Publication Date (Web): January 22, 2002 (Article)
DOI: 10.1021/jm010106k
Structural Aspects of Isozyme Selectivity in the Binding of Inhibitors to Carbonic Anhydrases II and IV
Chu-Young Kim, Douglas A. Whittington, Jeanne S. Chang, John Liao, Jesse A. May, and David W. Christianson
pp 888–893Publication Date (Web): January 17, 2002 (Article)
DOI: 10.1021/jm010163d
Kinetic Studies of the Binding of Acridinecarboxamide Topoisomerase Poisons to DNA: Implications for Mode of Binding of Ligands with Uncharged Chromophores
Laurence P. G. Wakelin, Adrienne Adams, and William A. Denny
pp 894–901Publication Date (Web): January 17, 2002 (Article)
DOI: 10.1021/jm000473g
Pyridophens: Binary Pyridostigmine−Aprophen Prodrugs with Differential Inhibition of Acetylcholinesterase, Butyrylcholinesterase, and Muscarinic Receptors
Haim Leader, Alan David Wolfe, Peter K. Chiang, and Richard K. Gordon
pp 902–910Publication Date (Web): January 11, 2002 (Article)
DOI: 10.1021/jm010196t
Cysteine Derivatives as Inhibitors for Carboxypeptidase A: Synthesis and Structure−Activity Relationships
Jung Dae Park and Dong H. Kim
pp 911–918Publication Date (Web): January 17, 2002 (Article)
DOI: 10.1021/jm010272s
New Type of Metalloproteinase Inhibitor: Design and Synthesis of New Phosphonamide-Based Hydroxamic Acids
Masaaki Sawa, Takao Kiyoi, Kiriko Kurokawa, Hiroshi Kumihara, Minoru Yamamoto, Tomohiro Miyasaka, Yasuko Ito, Ryoichi Hirayama, Tomomi Inoue, Yasuyuki Kirii, Eiji Nishiwaki, Hiroshi Ohmoto, Yu Maeda, Etsuko Ishibushi, Yoshimasa Inoue, Kohichiro Yoshino, and Hirosato Kondo
pp 919–929Publication Date (Web): January 15, 2002 (Article)
DOI: 10.1021/jm0103211
New Strategy for Antedrug Application: Development of Metalloproteinase Inhibitors as Antipsoriatic Drugs
Masaaki Sawa, Takako Tsukamoto, Takao Kiyoi, Kiriko Kurokawa, Fumio Nakajima, Yuichiro Nakada, Koichi Yokota, Yoshimasa Inoue, Hirosato Kondo, and Kohichiro Yoshino
pp 930–936Publication Date (Web): January 15, 2002 (Article)
DOI: 10.1021/jm010349c
Synthesis and Biological Activity of the Prodrug of Class I Major Histocompatibility Peptide GILGFVFTL Activated by β-Glucuronidase1
Sharad Rawale, Lew M. Hrihorczuk, Wei-Zen Wei, and Jiri Zemlicka
pp 937–943Publication Date (Web): January 16, 2002 (Article)
DOI: 10.1021/jm010352w
N-Aryl N‘-Hydroxyguanidines, A New Class of NO-Donors after Selective Oxidation by Nitric Oxide Synthases: Structure−Activity Relationship
Axelle Renodon-Cornière, Sylvie Dijols, Céline Perollier, David Lefevre-Groboillot, Jean-Luc Boucher, Roger Attias, Marie-Agnes Sari, Dennis Stuehr, and Daniel Mansuy
pp 944–954Publication Date (Web): December 27, 2001 (Article)
DOI: 10.1021/jm011006h
Syntheses, Calcium Channel Agonist−Antagonist Modulation Activities, Nitric Oxide Release, and Voltage-Clamp Studies of 2-Nitrooxyethyl 1,4-Dihydro- 2,6-dimethyl-3-nitro-4-(2-trifluoromethylphenyl)pyridine-5-carboxylate Enantiomers
Rudong Shan, Susan E. Howlett, and Edward E. Knaus
pp 955–961Publication Date (Web): January 22, 2002 (Article)
DOI: 10.1021/jm010394k
Novel Antagonists Acting at the P2Y1 Purinergic Receptor: Synthesis and Conformational Analysis Using Potentiometric and Nuclear Magnetic Resonance Titration Techniques
Pierre Raboisson, Anthony Baurand, Jean-Pierre Cazenave, Christian Gachet, Myriam Retat, Bernard Spiess, and Jean-Jacques Bourguignon
pp 962–972Publication Date (Web): January 12, 2002 (Article)
DOI: 10.1021/jm0104062
Computational Studies on Tetrahydropyrimidine-2-one HIV-1 Protease Inhibitors: Improving Three-Dimensional Quantitative Structure−Activity Relationship Comparative Molecular Field Analysis Models by Inclusion of Calculated Inhibitor- and Receptor-Based Properties
Anil C. Nair, Philippa Jayatilleke, Xia Wang, Stanislav Miertus, and William J. Welsh
pp 973–983Publication Date (Web): January 17, 2002 (Article)
DOI: 10.1021/jm010417v
Brief Articles
Cyclohexylmethylpiperidinyltriphenylpropioamide: A Selective Muscarinic M3 Antagonist Discriminating against the Other Receptor Subtypes
Yufu Sagara, Takeshi Sagara, Toshiaki Mase, Toshifumi Kimura, Tomoshige Numazawa, Toru Fujikawa, Kazuhito Noguchi, and Norikazu Ohtake
pp 984–987Publication Date (Web): January 18, 2002 (Brief Article)
DOI: 10.1021/jm010480k
Selective Antagonists at Group I Metabotropic Glutamate Receptors: Synthesis and Molecular Pharmacology of 4-Aryl-3-isoxazolol Amino Acids
Hasse Kromann, Frank A. Sløk, Tine B. Stensbøl, Hans Bräuner-Osborne, Ulf Madsen, and Povl Krogsgaard-Larsen
pp 988–991Publication Date (Web): January 11, 2002 (Brief Article)
DOI: 10.1021/jm010443t
Book Reviews
Medicinal Chemistry into the Millennium Edited by M. M. Campbell and I. S. Blagbrough. The Royal Society of Chemistry, Cambridge, U.K. 2001. x + 398 pp. 16 × 24 cm. ISBN 0-854-04-769-7. £69.50.
Manfred E. Wolff
p 992Publication Date (Web): December 15, 2001 (Book Review)
DOI: 10.1021/jm010445d
The Sigma-RBI Handbook of Receptor Classification and Signal Transduction. Fourth Edition Edited by Keith J. Watling. Sigma-RBI, Natick, MA. 2001. viii + 231 pp. 28 × 23 cm. ISBN 0-9640548-3-3. $55.00.
Joseph G. Cannon
pp 992–993Publication Date (Web): December 22, 2001 (Book Review)
DOI: 10.1021/jm0105124
Quantitative Chromatographic Analysis. Volume 85 By Thomas Beesley, Benjamin Buglio, and P. W. Scott. Marcel Dekker, New York, 2001. xx + 378 pp. 15 × 23 cm. ISBN 0-8247-0503-3. $150.00.
Jerry L. Born
p 993Publication Date (Web): January 18, 2002 (Book Review)
DOI: 10.1021/jm010514o
Advances in Chromatography. Volume 41 Edited by Phyllis R. Brown and Eli Grushka. Marcel Dekker, New York. 2001. xx + 425 pp. 15 × 23 cm. ISBN 0-8247-0509-2. $195.00.
Jerry L. Born
p 993Publication Date (Web): January 18, 2002 (Book Review)
DOI: 10.1021/jm010515g
The Handbook of Nucleoside Synthesis By Helmut Vorbrüggen and Carmen Ruh-Pohlenz. John Wiley & Sons, New York. 2001. xii + 631 pp. 15.5 × 23 cm. ISBN 0-471-09383-1 (paper). $79.95.
Donald E. Bergstrom
pp 993–994Publication Date (Web): January 16, 2002 (Book Review)
DOI: 10.1021/jm010545j