Table of Contents
August 14, 2003
Volume 46, Issue 17
Pages 3559-3770
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).
Letters
Autoradiographic Visualization of Corticotropin Releasing Hormone Type 1 Receptors with a Nonpeptide Ligand: Synthesis of [76Br]MJL-1-109-2
Elaine Jagoda, Carlo Contoreggi, Mei-Jing Lee, Chih-Hao K. Kao, Lawrence P. Szajek, Sam Listwak, Philip Gold, George Chrousos, Elisabeth Greiner, B. Moon Kim, Arthur E. Jacobson, Kenner C. Rice, and William Eckelman
pp 3559–3562Publication Date (Web): July 16, 2003 (Letter)
DOI: 10.1021/jm034077k
Hi-Res PDFAntimalarial Drug Quinacrine Binds to C-Terminal Helix of Cellular Prion Protein
Martin Vogtherr, Susanne Grimme, Bettina Elshorst, Doris M. Jacobs, Klaus Fiebig, Christian Griesinger, and Ralph Zahn
pp 3563–3564Publication Date (Web): July 11, 2003 (Letter)
DOI: 10.1021/jm034093h
Selective Formation of Homo- and Heterobivalent Peptidomimetics
Mookda Pattarawarapan, Samuel Reyes, Zebin Xia, Maria C. Zaccaro, H. Uri Saragovi, and Kevin Burgess
pp 3565–3567Publication Date (Web): July 15, 2003 (Letter)
DOI: 10.1021/jm034103e
Structure−Activity Relationships in Carboxamide Derivatives Based on the Targeted Delivery of Radionuclides and Boron Atoms by Means of Peripheral Benzodiazepine Receptor Ligands
Andrea Cappelli, Gal.la Pericot Mohr, Andrea Gallelli, Germano Giuliani, Maurizio Anzini, Salvatore Vomero, Massimo Fresta, Patrizia Porcu, Elisabetta Maciocco, Alessandra Concas, Giovanni Biggio, and Alessandro Donati
pp 3568–3571Publication Date (Web): July 18, 2003 (Letter)
DOI: 10.1021/jm034068b
Articles
Prediction of Aqueous Solubility of a Diverse Set of Compounds Using Quantitative Structure−Property Relationships
Ailan Cheng and Kenneth M. Merz, Jr.
pp 3572–3580Publication Date (Web): July 23, 2003 (Article)
DOI: 10.1021/jm020266b
Design, Synthesis, and Evaluation of Substituted Phenylpropanoic Acid Derivatives as Human Peroxisome Proliferator Activated Receptor Activators. Discovery of Potent and Human Peroxisome Proliferator Activated Receptor α Subtype-Selective Activators
Masahiro Nomura, Takahiro Tanase, Tomohiro Ide, Masaki Tsunoda, Masahiro Suzuki, Hideharu Uchiki, Koji Murakami, and Hiroyuki Miyachi
pp 3581–3599Publication Date (Web): July 10, 2003 (Article)
DOI: 10.1021/jm0205144
Functionalized Glycomers as Growth Inhibitors and Inducers of Apoptosis in Human Glioblastoma Cells
Stephen Hanessian, Lijie Zhan, Raymonde Bovey, Oscar M. Saavedra, and Lucienne Juillerat-Jeanneret
pp 3600–3611Publication Date (Web): July 16, 2003 (Article)
DOI: 10.1021/jm0205853
Efficacious and Orally Bioavailable Thrombin Inhibitors Based on a 2,5-Thienylamidine at the P1 Position: Discovery of N-Carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide
Koo Lee, Cheol Won Park, Won-Hyuk Jung, Hee Dong Park, Sun Hwa Lee, Kyung Ha Chung, Su Kyung Park, O Hwan Kwon, Myunggyun Kang, Doo-Hee Park, Sang Koo Lee, Eunice E. Kim, Suk Kyoon Yoon, and Aeri Kim
pp 3612–3622Publication Date (Web): July 12, 2003 (Article)
DOI: 10.1021/jm030025j
Synthesis of Novel Macrocyclic Docetaxel Analogues. Influence of Their Macrocyclic Ring Size on Tubulin Activity
Olivier Querolle, Joëlle Dubois, Sylviane Thoret, Fanny Roussi, Sara Montiel-Smith, Françoise Guéritte, and Daniel Guénard
pp 3623–3630Publication Date (Web): July 23, 2003 (Article)
DOI: 10.1021/jm030770w
Modeling of Human Cytochrome P450-Mediated Drug Metabolism Using Unsupervised Machine Learning Approach
Dmitry Korolev, Konstantin V. Balakin, Yuri Nikolsky, Eugene Kirillov, Yan A. Ivanenkov, Nikolay P. Savchuk, Andrey A. Ivashchenko, and Tatiana Nikolskaya
pp 3631–3643Publication Date (Web): July 23, 2003 (Article)
DOI: 10.1021/jm030102a
Structure-Based Design and Synthesis of Novel Potent Na+,K+-ATPase Inhibitors Derived from a 5α,14α-Androstane Scaffold as Positive Inotropic Compounds
Sergio De Munari, Alberto Cerri, Mauro Gobbini, Nicoletta Almirante, Leonardo Banfi, Giulio Carzana, Patrizia Ferrari, Giuseppe Marazzi, Rosella Micheletti, Antonio Schiavone, Simona Sputore, Marco Torri, Maria Pia Zappavigna, and Piero Melloni
pp 3644–3654Publication Date (Web): July 23, 2003 (Article)
DOI: 10.1021/jm030830y
Discovery of (3S)-Amino-(4R)-ethylpiperidinyl Quinolones as Potent Antibacterial Agents with a Broad Spectrum of Activity and Activity against Resistant Pathogens
X. Eric Hu, Nick K. Kim, Jeffrey L. Gray, Ji-In K. Almstead, William L. Seibel, and Benoit Ledoussal
pp 3655–3661Publication Date (Web): July 22, 2003 (Article)
DOI: 10.1021/jm030272n
Synthesis and Biological Evaluation of 3-Alkoxy Analogues of Flavone-8-acetic Acid
Silvia Gobbi, Angela Rampa, Alessandra Bisi, Federica Belluti, Lorna Piazzi, Piero Valenti, Anna Caputo, Antonella Zampiron, and Maria Carrara
pp 3662–3669Publication Date (Web): July 23, 2003 (Article)
DOI: 10.1021/jm030771o
Highly Potent 1,4-Benzothiazine Derivatives as KATP-Channel Openers1
Violetta Cecchetti, Vincenzo Calderone, Oriana Tabarrini, Stefano Sabatini, Enrica Filipponi, Lara Testai, Roberto Spogli, Enrica Martinotti, and Arnaldo Fravolini
pp 3670–3679Publication Date (Web): July 12, 2003 (Article)
DOI: 10.1021/jm030791q
Design and Synthesis of Novel Pyridoxine 5‘-Phosphonates as Potential Antiischemic Agents
Vinh Pham, Wenlian Zhang, Vince Chen, Tara Whitney, John Yao, Doug Froese, Albert D. Friesen, James M. Diakur, and Wasim Haque
pp 3680–3687Publication Date (Web): July 11, 2003 (Article)
DOI: 10.1021/jm0300678
Stereoselective Synthesis and Structure−Activity Relationship of Novel Ceramide Trafficking Inhibitors. (1R,3R)-N-(3-Hydroxy-1-hydroxymethyl-3-phenylpropyl)dodecanamide and Its Analogues
Yoshitaka Nakamura, Ryosuke Matsubara, Hidetoshi Kitagawa, Shū Kobayashi, Keigo Kumagai, Satoshi Yasuda, and Kentaro Hanada
pp 3688–3695Publication Date (Web): July 23, 2003 (Article)
DOI: 10.1021/jm0300779
Enantioselective Syntheses and Cytotoxicity of N,O-Nucleosides
Ugo Chiacchio, Antonino Corsaro, Daniela Iannazzo, Anna Piperno, Venerando Pistarà, Antonio Rescifina, Roberto Romeo, Vincenza Valveri, Antonio Mastino, and Giovanni Romeo
pp 3696–3702Publication Date (Web): July 04, 2003 (Article)
DOI: 10.1021/jm0308186
A Comparison of Phosphonothioic Acids with Phosphonic Acids as Phosphatase Inhibitors
Krzysztof Swierczek, Arti S. Pandey, John W. Peters, and Alvan C. Hengge
pp 3703–3708Publication Date (Web): July 18, 2003 (Article)
DOI: 10.1021/jm030106f
A Novel Class of Nonpeptidic Biaryl Inhibitors of Human Cathepsin K
Joël Robichaud, Renata Oballa, Peppi Prasit, Jean-Pierre Falgueyret, M. David Percival, Gregg Wesolowski, Sevgi B. Rodan, Donald Kimmel, Colena Johnson, Cliff Bryant, Shankar Venkatraman, Eduardo Setti, Rohan Mendonca, and James T. Palmer
pp 3709–3727Publication Date (Web): July 16, 2003 (Article)
DOI: 10.1021/jm0301078
Structure−Activity Relationships of Novel Cyclic α-MSH/β-MSH Hybrid Analogues That Lead to Potent and Selective Ligands for the Human MC3R and Human MC5R
Preeti Balse-Srinivasan, Paolo Grieco, Minying Cai, Dev Trivedi, and Victor J. Hruby
pp 3728–3733Publication Date (Web): July 23, 2003 (Article)
DOI: 10.1021/jm030111j
Water Soluble, Core-Modified Porphyrins. 3. Synthesis, Photophysical Properties, and in Vitro Studies of Photosensitization, Uptake, and Localization with Carboxylic Acid-Substituted Derivatives
Youngjae You, Scott L. Gibson, Russell Hilf, Sherry R. Davies, Allan R. Oseroff, Indrajit Roy, Tymish Y. Ohulchanskyy, Earl J. Bergey, and Michael R. Detty
pp 3734–3747Publication Date (Web): July 16, 2003 (Article)
DOI: 10.1021/jm030136i
Hydroxyurea Analogues As Kinetic and Mechanistic Probes of the Nitric Oxide Producing Reactions of Hydroxyurea and Oxyhemoglobin
Jinming Huang, Zhou Zou, Daniel B. Kim-Shapiro, Samir K. Ballas, and S. Bruce King
pp 3748–3753Publication Date (Web): July 18, 2003 (Article)
DOI: 10.1021/jm0301538
Brief Articles
Bispyridinium Cyclophanes: Novel Templates for Human Choline Kinase Inhibitors
Ana Conejo-García, Joaquín M. Campos, Rosario M. Sánchez-Martín, Miguel Á. Gallo, and Antonio Espinosa
pp 3754–3757Publication Date (Web): June 27, 2003 (Brief Article)
DOI: 10.1021/jm030792i
Synthesis and Evaluation of Pharmacological Properties of Novel Annelated 2,3-Benzodiazepine Derivatives
Rosaria Gitto, Valérie Orlando, Silvana Quartarone, Giovambattista De Sarro, Angela De Sarro, Emilio Russo, Guido Ferreri, and Alba Chimirri
pp 3758–3761Publication Date (Web): July 10, 2003 (Brief Article)
DOI: 10.1021/jm030821p
New Potential Uroselective NO-Donor α1-Antagonists
Donatella Boschi, Gian Cesare Tron, Antonella Di Stilo, Roberta Fruttero, Alberto Gasco, Elena Poggesi, Gianni Motta, and Amedeo Leonardi
pp 3762–3765Publication Date (Web): July 23, 2003 (Brief Article)
DOI: 10.1021/jm030825u
Conformationally Defined Retinoic Acid Analogues. 5. Large-Scale Synthesis and Mammary Cancer Chemopreventive Activity for (2E,4E,6Z,8E)-8- (3‘,4‘-Dihydro-1‘(2‘H)-naphthalen-1‘-ylidene)-3,7-dimethyl-2,4,6-octatrienoic Acid (9cUAB30)
Venkatram R. Atigadda, Kimberly K. Vines, Clinton J. Grubbs, Donald L. Hill, Samuel L. Beenken, Kirby I. Bland, Wayne J. Brouillette, and Donald D. Muccio
pp 3766–3769Publication Date (Web): July 23, 2003 (Brief Article)
DOI: 10.1021/jm030095q
Book Reviews
Amino Acid and Peptide Synthesis. Second Edition By John Jones. Oxford University Press, New York. 2002. 92 pp. 19 × 25 cm. ISBN 0-19-925738-8. $15.95.
D. Eric Walters
p 3770Publication Date (Web): July 18, 2003 (Book Review)
DOI: 10.1021/jm030261u