Table of Contents
December 15, 2005
Volume 48, Issue 25
Pages 7919-8102
About the Cover: Illustration of the binding mode of a biheteroaryl inhibitor to vascular endothelial growth factor receptor-2 (Kuo, G.-H.; et al. J. Med. Chem. 2005, 48, 1886-1900).
Letters
First Structure−Activity Relationship Study on Dopamine D3 Receptor Agents with N-[4-(4-Arylpiperazin-1-yl)butyl]arylcarboxamide Structure
Marcello Leopoldo, Enza Lacivita, Nicola A. Colabufo, Marialessandra Contino, Francesco Berardi, and Roberto Perrone
pp 7919–7922Publication Date (Web): November 18, 2005 (Letter)
DOI: 10.1021/jm050729o
Hi-Res PDFDifferent Stereochemical Requirements for CXCR4 Binding and Signaling Functions As Revealed by an Anti-HIV, d-Amino Acid-Containing SMM-Chemokine Ligand
Chang-Zhi Dong, Santosh Kumar, Won-Tak Choi, Navid Madani, Shaomin Tian, Jing An, Joseph G. Sodroski, and Ziwei Huang
pp 7923–7924Publication Date (Web): November 19, 2005 (Letter)
DOI: 10.1021/jm050829u
Articles
Antitumoral Activity of Non-Platinum Xanthate Complexes
Wolfgang Friebolin, Gerhard Schilling, Margot Zöller, and Eberhard Amtmann
pp 7925–7931Publication Date (Web): November 19, 2005 (Article)
DOI: 10.1021/jm040899l
1,2,4-Triazolo[1,5-a]quinoxaline as a Versatile Tool for the Design of Selective Human A3 Adenosine Receptor Antagonists: Synthesis, Biological Evaluation, and Molecular Modeling Studies of 2-(Hetero)aryl- and 2-Carboxy-Substitued Derivatives
Daniela Catarzi, Vittoria Colotta, Flavia Varano, Ombretta Lenzi, Guido Filacchioni, Letizia Trincavelli, Claudia Martini, Christian Montopoli, and Stefano Moro
pp 7932–7945Publication Date (Web): November 11, 2005 (Article)
DOI: 10.1021/jm0504149
Comparative Virtual and Experimental High-Throughput Screening for Glycogen Synthase Kinase-3β Inhibitors
Tímea Polgár, Andrea Baki, Györgyi I. Szendrei, and György M. Keserűu
pp 7946–7959Publication Date (Web): November 12, 2005 (Article)
DOI: 10.1021/jm050504d
Use of Structure-Based Drug Design Approaches to Obtain Novel Anthranilic Acid Acyl Carrier Protein Synthase Inhibitors
Diane Joseph-McCarthy, Kevin Parris, Adrian Huang, Amedeo Failli, Dominick Quagliato, Elizabeth Glasfeld Dushin, Elena Novikova, Elena Severina, Margareta Tuckman, Peter J. Petersen, Charles Dean, Christian C. Fritz, Tova Meshulam, Maureen DeCenzo, Larry Dick, Iain J. McFadyen, William S. Somers, Frank Lovering, and Adam M. Gilbert
pp 7960–7969Publication Date (Web): November 16, 2005 (Article)
DOI: 10.1021/jm050523n
Further Structure−Activity Relationship Studies of Piperidine-Based Monoamine Transporter Inhibitors: Effects of Piperidine Ring Stereochemistry on Potency. Identification of Norepinephrine Transporter Selective Ligands and Broad-Spectrum Transporter Inhibitors
Rong He, Toru Kurome, Kelly M. Giberson, Kenneth M. Johnson, and Alan P. Kozikowski
pp 7970–7979Publication Date (Web): November 17, 2005 (Article)
DOI: 10.1021/jm050694s
Chemoenzymatic Synthesis of a Series of 4-Substituted Glutamate Analogues and Pharmacological Characterization at Human Glutamate Transporters Subtypes 1−3
Sebastien Alaux, Mie Kusk, Emanuelle Sagot, Jean Bolte, Anders A. Jensen, Hans Bräuner-Osborne, Thierry Gefflaut, and Lennart Bunch
pp 7980–7992Publication Date (Web): November 10, 2005 (Article)
DOI: 10.1021/jm050597z
N-Picolyl Derivatives of Kemp's Triamine as Potential Antitumor Agents: A Preliminary Investigation
Celeste Aida S. Regino, Suzy V. Torti, Rong Ma, Glenn P. A. Yap, Kevin A. Kreisel, Frank M. Torti, Roy P. Planalp, and Martin W. Brechbiel
pp 7993–7999Publication Date (Web): November 10, 2005 (Article)
DOI: 10.1021/jm050724r
Parallel Solution-Phase and Microwave-Assisted Synthesis of New S-DABO Derivatives Endowed with Subnanomolar Anti-HIV-1 Activity
Fabrizio Manetti, José A. Esté, Imma Clotet-Codina, Mercedes Armand-Ugón, Giovanni Maga, Emmanuele Crespan, Reynel Cancio, Claudia Mugnaini, Cesare Bernardini, Andrea Togninelli, Caterina Carmi, Maddalena Alongi, Elena Petricci, Silvio Massa, Federico Corelli, and Maurizio Botta
pp 8000–8008Publication Date (Web): November 11, 2005 (Article)
DOI: 10.1021/jm050744t
Diketo Acid Pharmacophore. 2. Discovery of Structurally Diverse Inhibitors of HIV-1 Integrase
Raveendra Dayam, Tino Sanchez, and Nouri Neamati
pp 8009–8015Publication Date (Web): November 15, 2005 (Article)
DOI: 10.1021/jm050837a
Effects of Variable Docking Conditions and Scoring Functions on Corresponding Protein-Aligned Comparative Molecular Field Analysis Models Constructed from Diverse Human Protein Tyrosine Phosphatase 1B Inhibitors
Mutasem O. Taha and Murad A. AlDamen
pp 8016–8034Publication Date (Web): November 15, 2005 (Article)
DOI: 10.1021/jm058047o
Potent Dmt-Tic Pharmacophoric δ- and μ-Opioid Receptor Antagonists
Tingyou Li, Yoshio Fujita, Kimitaka Shiotani, Anna Miyazaki, Yuko Tsuda, Akihiro Ambo, Yusuke Sasaki, Yunden Jinsmaa, Ewa Marczak, Sharon D. Bryant, Severo Salvadori, Lawrence H. Lazarus, and Yoshio Okada,
pp 8035–8044Publication Date (Web): November 03, 2005 (Article)
DOI: 10.1021/jm050377l
Discovery of Indoles as Potent and Selective Inhibitors of the Deacetylase SIRT1
Andrew D. Napper, Jeffrey Hixon, Thomas McDonagh, Kenneth Keavey, Jean-Francois Pons, Jonathan Barker, Wei Tsung Yau, Patricia Amouzegh, Adam Flegg, Estelle Hamelin, Russell J. Thomas, Michael Kates, Stephen Jones, Manuel A. Navia, Jeffrey O. Saunders, Peter S. DiStefano, and Rory Curtis
pp 8045–8054Publication Date (Web): November 09, 2005 (Article)
DOI: 10.1021/jm050522v
New Bradykinin Analogues Modified in the C-Terminal Part with Sterically Restricted 1-Aminocyclohexane-1-carboxylic Acid
Olga Labudda-Dawidowska, Tomasz H. Wierzba, Adam Prahl, Wioleta Kowalczyk, Łukasz Gawiński, Marketa Plackova, Jiřina Slaninová, and Bernard Lammek
pp 8055–8059Publication Date (Web): November 16, 2005 (Article)
DOI: 10.1021/jm0580353
Synthesis and Characterization of Platinum(IV) Anticancer Drugs with Functionalized Aromatic Carboxylate Ligands: Influence of the Ligands on Drug Efficacies and Uptake
Wee Han Ang, Sébastien Pilet, Rosario Scopelliti, François Bussy, Lucienne Juillerat-Jeanneret, and Paul J. Dyson
pp 8060–8069Publication Date (Web): November 01, 2005 (Article)
DOI: 10.1021/jm0506468
Synthesis and Biological Evaluation of a Novel Series of “Ortho-Nitrated” Inhibitors of Catechol-O-methyltransferase
David A. Learmonth, Maria João Bonifácio, and Patrício Soares-da-Silva
pp 8070–8078Publication Date (Web): November 17, 2005 (Article)
DOI: 10.1021/jm0580454
cycloSal-PMEA and cycloAmb-PMEA: Potentially New Phosphonate Prodrugs Based on the cycloSal-Pronucleotide Approach
Chris Meier, Ulf Görbig, Christian Müller, and Jan Balzarini
pp 8079–8086Publication Date (Web): November 10, 2005 (Article)
DOI: 10.1021/jm050641a
Antitrypanosomal, Antileishmanial, and Antimalarial Activities of Quaternary Arylalkylammonium 2-Amino-4-Chlorophenyl Phenyl Sulfides, a New Class of Trypanothione Reductase Inhibitor, and of N-Acyl Derivatives of 2-Amino-4-Chlorophenyl Phenyl Sulfide
Seheli Parveen, Mohammed O. F. Khan, Susan E. Austin, Simon L. Croft, Vanessa Yardley, Peter Rock, and Kenneth T. Douglas
pp 8087–8097Publication Date (Web): November 09, 2005 (Article)
DOI: 10.1021/jm050819t
Brief Articles
A New Class of HIV-1 Protease Inhibitors Containing a Tertiary Alcohol in the Transition-State Mimicking Scaffold
Jenny K. Ekegren, Torsten Unge, Mayada Zreik Safa, Hans Wallberg, Bertil Samuelsson, and Anders Hallberg
pp 8098–8102Publication Date (Web): November 16, 2005 (Brief Article)
DOI: 10.1021/jm050790t