Table of Contents
September 23, 2004
Volume 47, Issue 20
Pages 4799-4978
About the Cover: RRibbon rendered illustration of the nuclear receptor heterodimer RXRα(cyan):PPARRγ (red) ligand binding domains bound with coactivator peptides (magenta) and agonist ligands (space-filling atoms where green is carbon, red is oxygen, and blue is nitrogen) (Haffner, C. D.; et al. J. Med. Chem. 2004, 47, 2010-2029).
Letters
Nonpeptidic, Noncovalent Inhibitors of the Cysteine Protease Cathepsin S
Robin L. Thurmond, Mary Pat Beavers, Hui Cai, Steven P. Meduna, Darin J. Gustin, Siquan Sun, Harold J. Almond, Lars Karlsson, and James P. Edwards
pp 4799–4801Publication Date (Web): August 20, 2004 (Letter)
DOI: 10.1021/jm0496133
Hi-Res PDFSynthesis of Taxoids with Improved Cytotoxicity and Solubility for Use in Tumor-Specific Delivery
Michael L. Miller, Elizabeth E. Roller, Robert Y. Zhao, Barbara A. Leece, Olga Ab, Erkan Baloglu, Victor S. Goldmacher, and Ravi V. J. Chari
pp 4802–4805Publication Date (Web): August 28, 2004 (Letter)
DOI: 10.1021/jm049705s
A Peptide Nucleic Acid−Neamine Conjugate That Targets and Cleaves HIV-1 TAR RNA Inhibits Viral Replication
Emmanuel Riguet, Snehlata Tripathi, Binay Chaubey, Jérôme Désiré, Virendra N. Pandey, and Jean-Luc Décout
pp 4806–4809Publication Date (Web): August 28, 2004 (Letter)
DOI: 10.1021/jm049642d
Entry into a New Class of Potent Proteasome Inhibitors Having High Antiproliferative Activity by Structure-Based Design
Pascal Furet, Patricia Imbach, Maria Noorani, Juergen Koeppler, Kurt Laumen, Marc Lang, Vito Guagnano, Peter Fuerst, Johannes Roesel, Johann Zimmermann, and Carlos García-Echeverría
pp 4810–4813Publication Date (Web): August 19, 2004 (Letter)
DOI: 10.1021/jm049660v
Synthesis and Photosensitizing Efficacy of Isomerically Pure Bacteriopurpurinimides
Yihui Chen, Adam Sumlin, Janet Morgan, Amy Gryshuk, Allan Oseroff, Barbara W. Henderson, Thomas J. Dougherty, and Ravindra K. Pandey
pp 4814–4817Publication Date (Web): August 28, 2004 (Letter)
DOI: 10.1021/jm049630s
Articles
Efficient Method for High-Throughput Virtual Screening Based on Flexible Docking: Discovery of Novel Acetylcholinesterase Inhibitors
Miho Yamada Mizutani and Akiko Itai
pp 4818–4828Publication Date (Web): July 23, 2008 (Article)
DOI: 10.1021/jm030605g
Nonpeptide αvβ3 Antagonists. Part 11: Discovery and Preclinical Evaluation of Potent αvβ3 Antagonists for the Prevention and Treatment of Osteoporosis
Paul J. Coleman, Karen M. Brashear, Ben C. Askew, John H. Hutchinson, Carol A. McVean, Le T. Duong, Bradley P. Feuston, Carmen Fernandez-Metzler, Michael A. Gentile, George D. Hartman, Donald B. Kimmel, Chih-Tai Leu, Lorraine Lipfert, Kara Merkle, Brenda Pennypacker, Thomayant Prueksaritanont, Gideon A. Rodan, Gregg A. Wesolowski, Sevgi B. Rodan, and Mark E. Duggan
pp 4829–4837Publication Date (Web): August 26, 2004 (Article)
DOI: 10.1021/jm049874c
Comparing the Conformational Behavior of a Series of Diastereomeric Cyclic Urea HIV-1 Inhibitors Using the Low Mode:Monte Carlo Conformational Search Method
Carol A. Parish, Matthew Yarger, Kent Sinclair, Myrianne Dure, and Alla Goldberg
pp 4838–4850Publication Date (Web): August 31, 2004 (Article)
DOI: 10.1021/jm049716l
NMR-Driven Discovery of Benzoylanthranilic Acid Inhibitors of Far Upstream Element Binding Protein Binding to the Human Oncogene c-myc Promoter
Jeffrey R. Huth, Liping Yu, Irene Collins, Jamey Mack, Renaldo Mendoza, Binumol Isaac, Demetrios T. Braddock, Steven W. Muchmore, Kenneth M. Comess, Stephen W. Fesik, G. Marius Clore, David Levens, and Philip J. Hajduk
pp 4851–4857Publication Date (Web): August 28, 2004 (Article)
DOI: 10.1021/jm0497803
Conformationally Constrained Analogues of Diacylglycerol (DAG). 23. Hydrophobic Ligand−Protein Interactions versus Ligand−Lipid Interactions of DAG-Lactones with Protein Kinase C (PK-C)
Hirokazu Tamamura, Dina M. Sigano, Nancy E. Lewin, Megan L. Peach, Marc C. Nicklaus, Peter M. Blumberg, and Victor E. Marquez
pp 4858–4864Publication Date (Web): August 27, 2004 (Article)
DOI: 10.1021/jm049723+
Full Text HTMLExploring the Binding Mode of Semicarbazide-Sensitive Amine Oxidase/VAP-1: Identification of Novel Substrates with Insulin-like Activity
Luc Marti, Anna Abella, Xavier de la Cruz, Silvia García-Vicente, Mercedes Unzeta, Christian Carpéné, Manuel Palacín, Xavier Testar, Modesto Orozco, and Antonio Zorzano
pp 4865–4874Publication Date (Web): August 28, 2004 (Article)
DOI: 10.1021/jm0499211
Novel Cyclooxygenase-1 Inhibitors Discovered Using Affinity Fingerprints
Nancy Hsu, Danying Cai, Komath Damodaran, Reinaldo F. Gomez, James G. Keck, Edgardo Laborde, Robert T. Lum, Thomas J. Macke, Graeme Martin, Steven R. Schow, Reyna J. Simon, Hugo O. Villar, Michael M. Wick, and Paul Beroza
pp 4875–4880Publication Date (Web): August 19, 2004 (Article)
DOI: 10.1021/jm049950b
Novel Synthesis of 3,4-Diarylisoxazole Analogues of Valdecoxib: Reversal Cyclooxygenase-2 Selectivity by Sulfonamide Group Removal
Leonardo Di Nunno, Paola Vitale, Antonio Scilimati, Stefania Tacconelli, and Paola Patrignani
pp 4881–4890Publication Date (Web): August 26, 2004 (Article)
DOI: 10.1021/jm040782x
Assessment of the Consistency of Medicinal Chemists in Reviewing Sets of Compounds
Michael S. Lajiness, Gerald M. Maggiora, and Veerabahu Shanmugasundaram
pp 4891–4896Publication Date (Web): August 21, 2004 (Article)
DOI: 10.1021/jm049740z
Reversible PEGylation: A Novel Technology To Release Native Interferon α2 over a Prolonged Time Period
Tal Peleg-Shulman, Haim Tsubery, Marina Mironchik, Mati Fridkin, Gideon Schreiber, and Yoram Shechter
pp 4897–4904Publication Date (Web): August 25, 2004 (Article)
DOI: 10.1021/jm0497693
Resistance-Modifying Agents. 11.1 Pyrimido[5,4-d]pyrimidine Modulators of Antitumor Drug Activity. Synthesis and Structure−Activity Relationships for Nucleoside Transport Inhibition and Binding to α1-Acid Glycoprotein
Nicola J. Curtin, Hannah C. Barlow, Karen J. Bowman, A. Hilary Calvert, Richard Davison, Bernard T. Golding, Bing Huang, Peter J. Loughlin, David R. Newell, Peter G. Smith, and Roger J. Griffin
pp 4905–4922Publication Date (Web): August 26, 2004 (Article)
DOI: 10.1021/jm040772w
Design, Synthesis, and Biological Evaluation of Biotin Conjugates of 2-Cyano-3,12-dioxooleana-1,9(11)-dien-28-oic Acid for the Isolation of the Protein Targets
Tadashi Honda, Tomasz Janosik, Yukiko Honda, Jie Han, Karen T. Liby, Charlotte R. Williams, Robin D. Couch, Amy C. Anderson, Michael B. Sporn, and Gordon W. Gribble
pp 4923–4932Publication Date (Web): August 18, 2004 (Article)
DOI: 10.1021/jm049727e
Synthesis and Biological Evaluation of New Acinetoferrin Homologues for Use as Iron Transport Probes in Mycobacteria
Richard A. Gardner, George Ghobrial, Saleh A. Naser, and Otto Phanstiel, IV
pp 4933–4940Publication Date (Web): August 26, 2004 (Article)
DOI: 10.1021/jm049805y
Macrocyclic Inhibitors for Peptide Deformylase: A Structure−Activity Relationship Study of the Ring Size
Xubo Hu, Kiet T. Nguyen, Vernon C. Jiang, Denene Lofland, Heinz E. Moser, and Dehua Pei
pp 4941–4949Publication Date (Web): August 24, 2004 (Article)
DOI: 10.1021/jm049592c
A Locally Active Antiinflammatory Macrolide (MLD987) for Inhalation Therapy of Asthma
Rene Hersperger, Karl-Heinz Buchheit, Salvatore Cammisuli, Albert Enz, Olivier Lohse, Monique Ponelle, Walter Schuler, Alain Schweitzer, Christoph Walker, Hartmut Zehender, Gerhard Zenke, Alfred G. Zimmerlin, Markus Zollinger, Lazzaro Mazzoni, and John R. Fozard
pp 4950–4957Publication Date (Web): August 31, 2004 (Article)
DOI: 10.1021/jm031101l
Synthesis, Electrochemistry, and Bioactivity of the Cyanobacterial Calothrixins and Related Quinones
Paul H. Bernardo, Christina L. L. Chai, Graham A. Heath, Peter J. Mahon, Geoffrey D. Smith, Paul Waring, and Bronwyn A. Wilkes
pp 4958–4963Publication Date (Web): August 27, 2004 (Article)
DOI: 10.1021/jm049625o
Antimitotic Activity of 5-Hydroxy-7-methoxy-2-phenyl-4-quinolones
Mohamed Hadjeri, Eva-Laure Peiller, Chantal Beney, Nabajyoti Deka, Martin A. Lawson, Charles Dumontet, and Ahcène Boumendjel
pp 4964–4970Publication Date (Web): August 26, 2004 (Article)
DOI: 10.1021/jm049876x
Brief Articles
Molecular Design of Cholesterols as Inhibitors of DNA Polymerase α
Masahiko Oshige, Kouji Kuramochi, Keisuke Ohta, Akitsu Ogawa, Hiroki Kuriyama, Fumio Sugawara, Susumu Kobayashi, and Kengo Sakaguchi
pp 4971–4974Publication Date (Web): August 11, 2004 (Brief Article)
DOI: 10.1021/jm030553v
Interaction between an Amantadine Analogue and the Transmembrane Portion of the Influenza A M2 Protein in Liposomes Probed by 1H NMR Spectroscopy of the Ligand
Antonios Kolocouris, Raino K. Hansen, and R. William Broadhurst
pp 4975–4978Publication Date (Web): August 28, 2004 (Brief Article)
DOI: 10.1021/jm0496685