Table of Contents
November 20, 2003
Volume 46, Issue 24
Pages 5097-5276
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
Histone Deacetylase Inhibitors
Thomas A. Miller, David J. Witter, and Sandro Belvedere
pp 5097–5116Publication Date (Web): October 28, 2003 (Perspective)
DOI: 10.1021/jm0303094
Hi-Res PDF Letters
A Novel Ergot Alkaloid as a 5-HT1A Inhibitor Produced by Dicyma sp.
María J. Vázquez, Ana M. Roa, Fernando Reyes, Alfonso Vega, Alfonso Rivera-Sagredo, David R. Thomas, Emilio Díez, and Juan A. Hueso-Rodríguez
pp 5117–5120Publication Date (Web): October 23, 2003 (Letter)
DOI: 10.1021/jm0341204
Design and Synthesis of a Potent and Selective Triazolone-Based Peroxisome Proliferator-Activated Receptor α Agonist
Yanping Xu, Daniel Mayhugh, Ashraf Saeed, Xiaodong Wang, Richard C. Thompson, Samuel J. Dominianni, Raymond F. Kauffman, Jaipal Singh, James S. Bean, William R. Bensch, Robert J. Barr, John Osborne, Chahrzad Montrose-Rafizadeh, Richard W. Zink, Nathan P. Yumibe, Naijia Huang, Debra Luffer-Atlas, Deepa Rungta, Dale E. Maise, and Nathan B. Mantlo
pp 5121–5124Publication Date (Web): October 18, 2003 (Letter)
DOI: 10.1021/jm034173l
Comparing Performance of Computational Tools for Combinatorial Library Design
Erik Evensen, John E. Eksterowicz, Robert V. Stanton, Connie Oshiro, Peter D. J. Grootenhuis, and Erin K. Bradley
pp 5125–5128Publication Date (Web): October 18, 2003 (Letter)
DOI: 10.1021/jm025618t
Articles
Defining the Molecular Requirements for the Selective Delivery of Polyamine Conjugates into Cells Containing Active Polyamine Transporters
Chaojie Wang, Jean-Guy Delcros, Laura Cannon, Fanta Konate, Horacio Carias, John Biggerstaff, Richard Andrew Gardner, and Otto Phanstiel IV
pp 5129–5138Publication Date (Web): October 18, 2003 (Article)
DOI: 10.1021/jm030223a
An Aromatic Microdomain at the Cannabinoid CB1 Receptor Constitutes an Agonist/Inverse Agonist Binding Region
Sean D. McAllister, Gulrukh Rizvi, Sharon Anavi-Goffer, Dow P. Hurst, Judy Barnett-Norris, Diane L. Lynch, Patricia H. Reggio, and Mary E. Abood
pp 5139–5152Publication Date (Web): October 23, 2003 (Article)
DOI: 10.1021/jm0302647
More Lipophilic Dialkyldiamine-Based Diazeniumdiolates: Synthesis, Characterization, and Application in Preparing Thromboresistant Nitric Oxide Release Polymeric Coatings
Melissa M. Batchelor, Sylvie L. Reoma, Paul S. Fleser, Vijay K. Nuthakki, Rose E. Callahan, Charles J. Shanley, Jeffrey K. Politis, Jessica Elmore, Scott I. Merz, and Mark E. Meyerhoff
pp 5153–5161Publication Date (Web): October 29, 2003 (Article)
DOI: 10.1021/jm030286t
Design and Synthesis of Novel Dimeric Morphinan Ligands for κ and μ Opioid Receptors
John L. Neumeyer, Ao Zhang, Wennan Xiong, Xiao-Hui Gu, James E. Hilbert, Brian I. Knapp, S. Stevens Negus, Nancy K. Mello, and Jean M. Bidlack
pp 5162–5170Publication Date (Web): October 25, 2003 (Article)
DOI: 10.1021/jm030139v
3-D QSAR Investigations of the Inhibition of Leishmania major Farnesyl Pyrophosphate Synthase by Bisphosphonates
John M. Sanders, Aurora Ortiz Gómez, Junhong Mao, Gary A. Meints, Erin M. Van Brussel, Agnieszka Burzynska, Pawel Kafarski, Dolores González-Pacanowska, and Eric Oldfield
pp 5171–5183Publication Date (Web): October 21, 2003 (Article)
DOI: 10.1021/jm0302344
Requirements for Specific Binding of Low Affinity Inhibitor Fragments to the SH2 Domain of pp60Src Are Identical to Those for High Affinity Binding of Full Length Inhibitors
Gudrun Lange, Dominique Lesuisse, Pierre Deprez, Bernard Schoot, Petra Loenze, Didier Bénard, Jean-Pierre Marquette, Pierre Broto, Edoardo Sarubbi, and Eliane Mandine
pp 5184–5195Publication Date (Web): October 28, 2003 (Article)
DOI: 10.1021/jm020970s
Dimerization Inhibitors of HIV-1 Protease Based on a Bicyclic Guanidinium Subunit
Perla Breccia, Nicole Boggetto, Ruth Pérez-Fernández, Michiel Van Gool, Masayuki Takahashi, Loïc René, Pilar Prados, Bernard Badet, Michèle Reboud-Ravaux, and Javier de Mendoza
pp 5196–5207Publication Date (Web): October 23, 2003 (Article)
DOI: 10.1021/jm030871u
Synthesis, Activity, and Molecular Modeling Studies of Novel Human Aldose Reductase Inhibitors Based on a Marine Natural Product
Jesús Ángel de la Fuente, Sonia Manzanaro, María Jesús Martín, Teresa G. de Quesada, Isabel Reymundo, Santos M. Luengo, and Federico Gago
pp 5208–5221Publication Date (Web): October 18, 2003 (Article)
DOI: 10.1021/jm030957n
Thiothalidomides: Novel Isosteric Analogues of Thalidomide with Enhanced TNF-α Inhibitory Activity
Xiaoxiang Zhu, Tony Giordano, Qian-sheng Yu, Harold W. Holloway, Tracy Ann Perry, Debomoy K. Lahiri, Arnold Brossi, and Nigel H. Greig
pp 5222–5229Publication Date (Web): October 16, 2003 (Article)
DOI: 10.1021/jm030152f
Synthesis and Preliminary Biological Evaluations of Ionic and Nonionic Amphiphilic α-Phenyl-N-tert-butylnitrone Derivatives
Grégory Durand, Ange Polidori, Olivier Ouari, Paul Tordo, Vanna Geromel, Pierre Rustin, and Bernard Pucci
pp 5230–5237Publication Date (Web): October 25, 2003 (Article)
DOI: 10.1021/jm030873e
Optically Active Mexiletine Analogues as Stereoselective Blockers of Voltage-Gated Na+ Channels
Carlo Franchini, Alessia Carocci, Alessia Catalano, Maria M. Cavalluzzi, Filomena Corbo, Giovanni Lentini, Antonio Scilimati, Paolo Tortorella, Diana Conte Camerino, and Annamaria De Luca
pp 5238–5248Publication Date (Web): October 31, 2003 (Article)
DOI: 10.1021/jm030865y
5,6,7-Trisubstituted 4-Aminopyrido[2,3-d]pyrimidines as Novel Inhibitors of Adenosine Kinase
Richard J. Perner, Yu-Gui Gu, Chih-Hung Lee, Erol K. Bayburt, Jeffery McKie, Karen M. Alexander, Kathy L. Kohlhaas, Carol T. Wismer, Joe Mikusa, Michael F. Jarvis, Elizabeth A. Kowaluk, and Shripad S. Bhagwat
pp 5249–5257Publication Date (Web): October 21, 2003 (Article)
DOI: 10.1021/jm030327l
Rational Design and Synthesis of Androgen Receptor-Targeted Nonsteroidal Anti-Androgen Ligands for the Tumor-Specific Delivery of a Doxorubicin−Formaldehyde Conjugate
Peter S. Cogan and Tad H. Koch
pp 5258–5270Publication Date (Web): October 18, 2003 (Article)
DOI: 10.1021/jm0303305
Synthesis of Second-Generation Transition State Analogues of Human Purine Nucleoside Phosphorylase
Gary B. Evans, Richard H. Furneaux, Andrzej Lewandowicz, Vern L. Schramm, and Peter C. Tyler
pp 5271–5276Publication Date (Web): October 23, 2003 (Article)
DOI: 10.1021/jm030305z