Table of Contents
November 6, 2003
Volume 46, Issue 23
Pages 4805-5095
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
Multidrug Resistance Reversal Agents
Jacques Robert and Christian Jarry
pp 4805–4817Publication Date (Web): October 10, 2003 (Perspective)
DOI: 10.1021/jm030183a
Hi-Res PDFNitroaryl Phosphoramides as Novel Prodrugs for E. coli Nitroreductase Activation in Enzyme Prodrug Therapy
Longqin Hu, Chengzhi Yu, Yongying Jiang, Jiye Han, Zhuorong Li, Patrick Browne, Paul R. Race, Richard J. Knox, Peter F. Searle, and Eva I. Hyde
pp 4818–4821Publication Date (Web): October 10, 2003 (Letter)
DOI: 10.1021/jm034133h
Synthesis and Biological Evaluation of 2‘-Methyl Taxoids Derived from Baccatin III and 14β-OH-Baccatin III 1,14-Carbonate
Arturo Battaglia, Ralph J. Bernacki, Carlo Bertucci, Ezio Bombardelli, Samanta Cimitan, Cristiano Ferlini, Gabriele Fontana, Andrea Guerrini, and Antonella Riva
pp 4822–4825Publication Date (Web): October 15, 2003 (Letter)
DOI: 10.1021/jm034146v
Discovery of (Aryloxopropenyl)pyrrolyl Hydroxyamides as Selective Inhibitors of Class IIa Histone Deacetylase Homologue HD1-A
Antonello Mai, Silvio Massa, Riccardo Pezzi, Dante Rotili, Peter Loidl, and Gerald Brosch
pp 4826–4829Publication Date (Web): October 15, 2003 (Letter)
DOI: 10.1021/jm034167p
Dissociation of Antibacterial and Hemolytic Activities of an Amphipathic Peptide Antibiotic
Chuanguang Qin, Xiaofen Zhong, Xianzhang Bu, Na Lee Joyce Ng, and Zhihong Guo
pp 4830–4833Publication Date (Web): October 02, 2003 (Letter)
DOI: 10.1021/jm0341352
Identification of a Potent and Selective 5-HT6 Antagonist: One-Step Synthesis of (E)-3-(Benzenesulfonyl)-2- (methylsulfanyl)pyrido[1,2-a]pyrimidin- 4-ylidenamine from 2-(Benzenesulfonyl)-3,3- bis(methylsulfanyl)acrylonitrile
Yong-Jin Wu, Huan He, Shuanghua Hu, Yazhong Huang, Paul M. Scola, Katharine Grant-Young, Robert L. Bertekap, Dedong Wu, Qi Gao, Yi Li, Cheryl Klakouski, and Ryan S. Westphal
pp 4834–4837Publication Date (Web): October 11, 2003 (Letter)
DOI: 10.1021/jm034142q
Articles
Conformational Study of Lipophilic Ligands in Phospholipid Model Membrane Systems by Solution NMR
Jianxin Guo, Spiro Pavlopoulos, Xiaoyu Tian, Dai Lu, Spyros P. Nikas, De-Ping Yang, and Alexandros Makriyannis
pp 4838–4846Publication Date (Web): October 15, 2003 (Article)
DOI: 10.1021/jm020385r
Modeling the Adenosine Receptors: Comparison of the Binding Domains of A2A Agonists and Antagonists
Soo-Kyung Kim, Zhan-Guo Gao, Philippe Van Rompaey, Ariel S. Gross, Aishe Chen, Serge Van Calenbergh, and Kenneth A. Jacobson
pp 4847–4859Publication Date (Web): October 10, 2003 (Article)
DOI: 10.1021/jm0300431
Synthesis and Ca2+-Mobilizing Activity of Purine-Modified Mimics of Adenophostin A: A Model for the Adenophostin−Ins(1,4,5)P3 Receptor Interaction
Heidi J. Rosenberg, Andrew M. Riley, Alex J. Laude, Colin W. Taylor, and Barry V. L. Potter
pp 4860–4871Publication Date (Web): October 02, 2003 (Article)
DOI: 10.1021/jm030883f
Design, Synthesis, and Biological Evaluation of 6-Substituted-3-(4-methanesulfonylphenyl)-4-phenylpyran-2-ones: A Novel Class of Diarylheterocyclic Selective Cyclooxygenase-2 Inhibitors
P. N. Praveen Rao, Mohsen Amini, Huiying Li, Amgad G. Habeeb, and Edward E. Knaus
pp 4872–4882Publication Date (Web): September 30, 2003 (Article)
DOI: 10.1021/jm0302391
Large Dimeric Ligands with Favorable Pharmacokinetic Properties and Peroxisome Proliferator-Activated Receptor Agonist Activity in Vitro and in Vivo
Per Sauerberg, Paul S. Bury, John P. Mogensen, Heinz-Josef Deussen, Ingrid Pettersson, Jan Fleckner, Jan Nehlin, Klaus S. Frederiksen, Tatjana Albrektsen, Nanni Din, L. Anders Svensson, Lars Ynddal, Erik M. Wulff, and Lone Jeppesen
pp 4883–4894Publication Date (Web): October 10, 2003 (Article)
DOI: 10.1021/jm0309046
Prazosin-Related Compounds. Effect of Transforming the Piperazinylquinazoline Moiety into an Aminomethyltetrahydroacridine System on the Affinity for α1-Adrenoreceptors
Michela Rosini, Alessandra Antonello, Andrea Cavalli, Maria L. Bolognesi, Anna Minarini, Gabriella Marucci, Elena Poggesi, Amedeo Leonardi, and Carlo Melchiorre
pp 4895–4903Publication Date (Web): October 10, 2003 (Article)
DOI: 10.1021/jm030952q
Multivalent Antibiotics via Metal Complexes: Potent Divalent Vancomycins against Vancomycin-Resistant Enterococci
Bengang Xing, Chun-Wing Yu, Pak-Leung Ho, Kin-Hung Chow, Terence Cheung, Hongwei Gu, Zongwei Cai, and Bing Xu
pp 4904–4909Publication Date (Web): October 10, 2003 (Article)
DOI: 10.1021/jm030417q
Potent and Selective Inhibitors of Platelet-Derived Growth Factor Receptor Phosphorylation. 3. Replacement of Quinazoline Moiety and Improvement of Metabolic Polymorphism of 4-[4-(N-Substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline Derivatives
Kenji Matsuno, Junko Ushiki, Takashi Seishi, Michio Ichimura, Neill A. Giese, Jin-Chen Yu, Shusuke Takahashi, Shoji Oda, and Yuji Nomoto
pp 4910–4925Publication Date (Web): October 14, 2003 (Article)
DOI: 10.1021/jm020505v
Synthesis, Characterization, and Biological Properties of 8-Azido- and 8-Amino-Substituted 2‘,5‘-Oligoadenylates
Hiroaki Sawai, Atushi Hirano, Hiroyuki Mori, Kazuo Shinozuka, Beihua Dong, and Robert H. Silverman
pp 4926–4932Publication Date (Web): October 04, 2003 (Article)
DOI: 10.1021/jm030035k
Isoquine and Related Amodiaquine Analogues: A New Generation of Improved 4-Aminoquinoline Antimalarials
Paul M. O'Neill, Amira Mukhtar, Paul A. Stocks, Laura E. Randle, Stephen Hindley, Stephen A. Ward, Richard C. Storr, Jamie F. Bickley, Ian A. O'Neil, James L. Maggs, Ruth H. Hughes, Peter A. Winstanley, Patrick G. Bray, and B. Kevin Park
pp 4933–4945Publication Date (Web): September 30, 2003 (Article)
DOI: 10.1021/jm030796n
Synthesis, Characterization, and in Vitro Antitumor Activity of Osteotropic Diam(m)ineplatinum(II) Complexes Bearing a N,N-Bis(phosphonomethyl)glycine Ligand
Markus Galanski, Susanna Slaby, Michael A. Jakupec, and Bernhard K. Keppler
pp 4946–4951Publication Date (Web): October 15, 2003 (Article)
DOI: 10.1021/jm0308040
Design and Synthesis of trans-3-(2-(4-((3-(3-(5-Methyl-1,2,4-oxadiazolyl))- phenyl)carboxamido)cyclohexyl)ethyl)-7-methylsulfonyl-2,3,4,5-tetrahydro- 1H-3-benzazepine (SB-414796): A Potent and Selective Dopamine D3 Receptor Antagonist
Gregor J. Macdonald, Clive L. Branch, Michael S. Hadley, Christopher N. Johnson, David J. Nash, Alexander B. Smith, Geoffrey Stemp, Kevin M. Thewlis, Antonio K. K. Vong, Nigel E. Austin, Phillip Jeffrey, Kim Y. Winborn, Izzy Boyfield, Jim J. Hagan, Derek N. Middlemiss, Charlie Reavill, Graham J. Riley, Jeannette M. Watson, Martyn Wood, Steve G. Parker, and Charles R. Ashby Jr.
pp 4952–4964Publication Date (Web): October 15, 2003 (Article)
DOI: 10.1021/jm030817d
Structure−Activity Relationships of γ-MSH Analogues at the Human Melanocortin MC3, MC4, and MC5 Receptors. Discovery of Highly Selective hMC3R, hMC4R, and hMC5R Analogues
Preeti Balse-Srinivasan, Paolo Grieco, Minying Cai, Dev Trivedi, and Victor J. Hruby
pp 4965–4973Publication Date (Web): October 04, 2003 (Article)
DOI: 10.1021/jm030119t
2-Substitution of Adenine Nucleotide Analogues Containing a Bicyclo[3.1.0]hexane Ring System Locked in a Northern Conformation: Enhanced Potency as P2Y1 Receptor Antagonists
Hak Sung Kim, Michihiro Ohno, Bin Xu, Hea Ok Kim, Yongseok Choi, Xiao D. Ji, Savitri Maddileti, Victor E. Marquez, T. Kendall Harden, and Kenneth A. Jacobson
pp 4974–4987Publication Date (Web): October 14, 2003 (Article)
DOI: 10.1021/jm030127+
Full Text HTMLThree-Dimensional Quantitative Structure−Activity Relationship Analysis of Propafenone-Type Multidrug Resistance Modulators: Influence of Variable Selection on Test Set Predictivity
Romy Fleischer and Michael Wiese
pp 4988–5004Publication Date (Web): October 09, 2003 (Article)
DOI: 10.1021/jm030876r
Design, Synthesis, and SAR of Potent and Selective Dipeptide-Derived Inhibitors for Dipeptidyl Peptidases
Kristel Senten, Pieter Van der Veken, Ingrid De Meester, Anne-Marie Lambeir, Simon Scharpé, Achiel Haemers, and Koen Augustyns
pp 5005–5014Publication Date (Web): September 17, 2003 (Article)
DOI: 10.1021/jm0308803
Anti-Herpes Simplex Virus Activity of Substituted 1-Hydroxyacridones
Christopher T. Lowden and Kenneth F. Bastow
pp 5015–5020Publication Date (Web): September 30, 2003 (Article)
DOI: 10.1021/jm030206l
Poly(ethylene glycol) Transport Forms of Vancomycin: A Long-Lived Continuous Release Delivery System
Richard B. Greenwald, Hong Zhao, Jing Xia, and Anthony Martinez
pp 5021–5030Publication Date (Web): October 03, 2003 (Article)
DOI: 10.1021/jm030202g
CpG Oligonucleotides with Modified Termini and Nicked Dumbbell Structure Show Enhanced Immunostimulatory Activity
Sukunath Narayanan, Alexander H. Dalpke, Karsten Siegmund, Klaus Heeg, and Clemens Richert
pp 5031–5044Publication Date (Web): October 14, 2003 (Article)
DOI: 10.1021/jm030902l
Synthesis and Biological Evaluation of 5-Substituted Derivatives of the Potent Antiherpes Agent (north)-Methanocarbathymine
Pamela Russ, Pierre Schelling, Leonardo Scapozza, Gerd Folkers, Erik De Clercq, and Victor E. Marquez
pp 5045–5054Publication Date (Web): October 14, 2003 (Article)
DOI: 10.1021/jm030241s
A New Generation of N-Aryl-N‘-(1-alkyl-2-chloroethyl)ureas as Microtubule Disrupters: Synthesis, Antiproliferative Activity, and β-Tubulin Alkylation Kinetics
Emmanuelle Mounetou, Jean Legault, Jacques Lacroix, and René C.-Gaudreault
pp 5055–5063Publication Date (Web): October 14, 2003 (Article)
DOI: 10.1021/jm030908a
5-Substituted-2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]pyrimidines
Acyclic Nucleoside Phosphonate Analogues with Antiviral Activity
Dana Hocková, Antonín Holý, Milena Masojídková, Graciela Andrei, Robert Snoeck, Erik De Clercq, and Jan Balzarini
pp 5064–5073Publication Date (Web): October 15, 2003 (Article)
DOI: 10.1021/jm030932o
Synthesis and Biological Evaluation of 2,4-Diamino-6-(arylaminomethyl)pyrido[2,3-d]pyrimidines as Inhibitors of Pneumocystis carinii and Toxoplasma gondii Dihydrofolate Reductase and as Antiopportunistic Infection and Antitumor Agents1
Aleem Gangjee, Ona O. Adair, and Sherry F. Queener
pp 5074–5082Publication Date (Web): October 04, 2003 (Article)
DOI: 10.1021/jm030312n
Brief Articles
Synthesis, in Vitro Evaluation, and Intraocular Pressure Effects of Water-Soluble Prodrugs of Endocannabinoid Noladin Ether
Juha Juntunen, Jouko Vepsäläinen, Riku Niemi, Krista Laine, and Tomi Järvinen
pp 5083–5086Publication Date (Web): September 20, 2003 (Brief Article)
DOI: 10.1021/jm030877j
Molecular Docking Studies of Natural Cholinesterase-Inhibiting Steroidal Alkaloids from Sarcococca saligna
Zaheer-ul-haq, Bernd Wellenzohn, Klaus R. Liedl, and Bernd M. Rode
pp 5087–5090Publication Date (Web): October 01, 2003 (Brief Article)
DOI: 10.1021/jm0309194
Estrogenic Potential of 2-Alkyl-4-(thio)chromenone 6-O-Sulfamates: Potent Inhibitors of Human Steroid Sulfatase
Peter Nussbaumer, Anthony P. Winiski, and Andreas Billich
pp 5091–5094Publication Date (Web): September 23, 2003 (Brief Article)
DOI: 10.1021/jm030926s
Book Reviews
Medicinal Plants of the World. Volume I: Chemical Constituents, Traditional and Modern Uses. Second Edition By Ivan A. Ross. Humana Press, Totawa, NJ. 2003. xv + 489 pp. 16.5 × 26 cm. ISBN 1-58829-281-9. $99.50.
Govind J. Kapadia
p 5095Publication Date (Web): October 08, 2003 (Book Review)
DOI: 10.1021/jm030397s