Table of Contents
July 31, 2003
Volume 46, Issue 16
Pages 3425-3558
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).
Award Address
Antibiotic Glycosyltransferases: Antibiotic Maturation and Prospects for Reprogramming
Christopher Walsh, Caren L. Freel Meyers, and Heather C. Losey
pp 3425–3436Publication Date (Web): July 04, 2003 (Perspective)
DOI: 10.1021/jm030257i
Hi-Res PDF Letters
Selective Protein Tyrosine Phosphatase 1B Inhibitors: Targeting the Second Phosphotyrosine Binding Site with Non-Carboxylic Acid-Containing Ligands
Gang Liu, Zhili Xin, Heng Liang, Cele Abad-Zapatero, Philip J. Hajduk, David A. Janowick, Bruce G. Szczepankiewicz, Zhonghua Pei, Charles W. Hutchins, Stephen J. Ballaron, Michael A. Stashko, Thomas H. Lubben, Cathy E. Berg, Cristina M. Rondinone, James M. Trevillyan, and Michael R. Jirousek
pp 3437–3440Publication Date (Web): June 25, 2003 (Letter)
DOI: 10.1021/jm034088d
Identification of “Latent Hits” in Compound Screening Collections
Jordi Mestres and Gerrit H. Veeneman
pp 3441–3444Publication Date (Web): July 01, 2003 (Letter)
DOI: 10.1021/jm034078c
Synthesis and Potent Antileukemic Activities of N-Lactylsphingosine and N-Lactyldihydrosphingosine
Hideki Azuma, Ryoko Takao, Keiji Shikata, Hayato Niiro, Taro Tachibana, and Kenji Ogino
pp 3445–3447Publication Date (Web): July 03, 2003 (Letter)
DOI: 10.1021/jm030125p
Effect of Detergent on “Promiscuous” Inhibitors
Ali J. Ryan, Norman M. Gray, Peter N. Lowe, and Chun-wa Chung
pp 3448–3451Publication Date (Web): July 04, 2003 (Letter)
DOI: 10.1021/jm0340896
Fumagalone, a Reversible Inhibitor of Type 2 Methionine Aminopeptidase and Angiogenesis
Guochun Zhou, Chiawei W. Tsai, and Jun O. Liu
pp 3452–3454Publication Date (Web): July 09, 2003 (Letter)
DOI: 10.1021/jm0341103
Articles
Design and Synthesis of Dihydrofolate Reductase Inhibitors Encompassing a Bridging Ester Group. Evaluation in a Mouse Colitis Model
Malin Graffner-Nordberg, Meredith Fyfe, Ralph Brattsand, Björn Mellgård, and Anders Hallberg
pp 3455–3462Publication Date (Web): July 01, 2003 (Article)
DOI: 10.1021/jm021062y
Synthesis and Structure−Activity Relationship of a New Series of COX-2 Selective Inhibitors: 1,5-Diarylimidazoles
Carmen Almansa, José Alfón, Alberto F. de Arriba, Fernando L. Cavalcanti, Ignasi Escamilla, Luis A. Gómez, Agustí Miralles, Robert Soliva, Javier Bartrolí, Elena Carceller, Manuel Merlos, and Julián García-Rafanell
pp 3463–3475Publication Date (Web): June 25, 2003 (Article)
DOI: 10.1021/jm030765s
Intermolecular Interactions between Peptidic and Nonpeptidic Agonists and the Third Extracellular Loop of the Cholecystokinin 1 Receptor
Craig Giragossian, Elizabeth E. Sugg, Jerzy R. Szewczyk, and Dale F. Mierke
pp 3476–3482Publication Date (Web): July 08, 2003 (Article)
DOI: 10.1021/jm030144z
A Second-Generation 99mTechnetium Single Photon Emission Computed Tomography Agent That Provides in Vivo Images of the Dopamine Transporter in Primate Brain
Peter C. Meltzer, Paul Blundell, Thomas Zona, Lihua Yang, Hong Huang, Ali A. Bonab, Eli Livni, Alan Fischman, and Bertha K. Madras
pp 3483–3496Publication Date (Web): July 04, 2003 (Article)
DOI: 10.1021/jm0301484
Development of a Water-Soluble Matrix Metalloproteinase Inhibitor as an Intra-arterial Infusion Drug for Prevention of Restenosis after Angioplasty
Takeshi Masuda and Yasuhide Nakayama
pp 3497–3501Publication Date (Web): July 03, 2003 (Article)
DOI: 10.1021/jm020356g
Monofunctional Platinum Complexes Showing Potent Cytotoxicity against Human Liver Carcinoma Cell Line BEL-7402
Junyong Zhang, Xiaoyong Wang, Chao Tu, Jun Lin, Jian Ding, Liping Lin, Zheming Wang, Cheng He, Chunhua Yan, Xiaozeng You, and Zijian Guo
pp 3502–3507Publication Date (Web): July 04, 2003 (Article)
DOI: 10.1021/jm020593j
Stereoselective Preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a Potent and Orally Active Dual Neurokinin NK1/NK2 Receptor Antagonist
Marc Gerspacher, Christine Lewis, Howard A. Ball, Colin Howes, Natarajan Subramanian, Karin Ryffel, and John R. Fozard
pp 3508–3513Publication Date (Web): June 27, 2003 (Article)
DOI: 10.1021/jm030786m
A Potent, Selective Inhibitor of Matrix Metalloproteinase-3 for the Topical Treatment of Chronic Dermal Ulcers
M. Jonathan Fray, Roger P. Dickinson, John P. Huggins, and Nicholas L. Occleston
pp 3514–3525Publication Date (Web): July 04, 2003 (Article)
DOI: 10.1021/jm0308038
Synthesis and Pharmacological Characterization of a Series of Geometrically Constrained 5-HT2A/2C Receptor Ligands
James J. Chambers, Jason C. Parrish, Niels H. Jensen, Deborah M. Kurrasch-Orbaugh, Danuta Marona-Lewicka, and David E. Nichols
pp 3526–3535Publication Date (Web): July 04, 2003 (Article)
DOI: 10.1021/jm030064v
Synthesis and in Vitro Antitumor Activity of Phenanthrolin-7-one Derivatives, Analogues of the Marine Pyridoacridine Alkaloids Ascididemin and Meridine: Structure−Activity Relationship
Evelyne Delfourne, Robert Kiss, Laurent Le Corre, Frederic Dujols, Jean Bastide, Françoise Collignon, Brigitte Lesur, Armand Frydman, and Francis Darro
pp 3536–3545Publication Date (Web): July 04, 2003 (Article)
DOI: 10.1021/jm0308702
Synthesis and Biological Evaluation of Resveratrol and Analogues as Apoptosis-Inducing Agents
Marinella Roberti, Daniela Pizzirani, Daniele Simoni, Riccardo Rondanin, Riccardo Baruchello, Caterina Bonora, Filippo Buscemi, Stefania Grimaudo, and Manlio Tolomeo
pp 3546–3554Publication Date (Web): July 01, 2003 (Article)
DOI: 10.1021/jm030785u
Brief Articles
α1-Adrenoceptor Antagonists. 6.1 Structural Optimization of Pyridazinone−Arylpiperazines. Study of the Influence on Affinity and Selectivity of Cyclic Substituents at the Pyridazinone Ring and Alkoxy Groups at the Arylpiperazine Moiety
Laura Betti, Federico Corelli, Monia Floridi, Gino Giannaccini, Laura Maccari, Fabrizio Manetti, Giovannella Strappaghetti, and Maurizio Botta
pp 3555–3558Publication Date (Web): June 11, 2003 (Brief Article)
DOI: 10.1021/jm0307842