Table of Contents
May 22, 2003
Volume 46, Issue 11
Pages 2017-2260
Miniperspective
Understanding the Structure−Activity Relationship of the Human Ether-a-go-go-Related Gene Cardiac K+ Channel. A Model for Bad Behavior
Robert Pearlstein, Roy Vaz, and David Rampe
pp 2017–2022Publication Date (Web): April 29, 2003 (Perspective)
DOI: 10.1021/jm0205651
Hi-Res PDF LETTERS
Identification of 1-Arylmethyl-3- (2-aminoethyl)-5-aryluracil as Novel Gonadotropin-Releasing Hormone Receptor Antagonists
Yun-Fei Zhu, Timothy D. Gross, Zhiqiang Guo, Patrick J. Connors, Jr., Yinghong Gao, Fabio C. Tucci, R. Scott Struthers, Greg J. Reinhart, John Saunders, Ta Kung Chen, Anne L. Killam Bonneville, and Chen Chen
pp 2023–2026Publication Date (Web): April 26, 2003 (Letter)
DOI: 10.1021/jm034041s
Synthesis, Structure−Activity Relationship, and Biological Studies of Indolocarbazoles as Potent Cyclin D1-CDK4 Inhibitors
Guoxin Zhu, Scott E. Conner, Xun Zhou, Chuan Shih, Tiechao Li, Bryan D. Anderson, Harold B. Brooks, Robert Morris Campbell, Eileen Considine, Jack A. Dempsey, Margaret M. Faul, Cathy Ogg, Bharvin Patel, Richard M. Schultz, Charles D. Spencer, Beverly Teicher, and Scott A. Watkins
pp 2027–2030Publication Date (Web): April 19, 2003 (Letter)
DOI: 10.1021/jm0256169
Articles
3D QSAR Analyses-Guided Rational Design of Novel Ligands for the (α4)2(β2)3 Nicotinic Acetylcholine Receptor
Holger Gohlke, Simone Schwarz, Daniela Gündisch, Maria Cristina Tilotta, Alexander Weber, Thomas Wegge, and Gunther Seitz
pp 2031–2048Publication Date (Web): April 22, 2003 (Article)
DOI: 10.1021/jm020859m
Novel Cationic Transport Agents for Oligonucleotide Delivery into Primary Leukemic Cells
Jarmila Králová, Michal Dvořák, and Vladimír Král
pp 2049–2056Publication Date (Web): April 16, 2003 (Article)
DOI: 10.1021/jm021060d
Restricted Conformation Analogues of an Anthelmintic Cyclodepsipeptide
Fred E. Dutton, Byung H. Lee, Sandra S. Johnson, Eileen M. Coscarelli, and Pil H. Lee
pp 2057–2073Publication Date (Web): April 26, 2003 (Article)
DOI: 10.1021/jm020482k
Calculation of the Binding Affinity of β-Secretase Inhibitors Using the Linear Interaction Energy Method
Brett A. Tounge and Charles H. Reynolds
pp 2074–2082Publication Date (Web): April 26, 2003 (Article)
DOI: 10.1021/jm020513b
Binding Structures and Potencies of Oxidosqualene Cyclase Inhibitors with the Homologous Squalene−Hopene Cyclase
Alexander Lenhart, Dirk J. Reinert, Johannes D. Aebi, Henrietta Dehmlow, Oliver H. Morand, and Georg E. Schulz
pp 2083–2092Publication Date (Web): April 30, 2003 (Article)
DOI: 10.1021/jm0211218
Discovery and Structure−Activity Relationship of Oxalylarylaminobenzoic Acids as Inhibitors of Protein Tyrosine Phosphatase 1B
Gang Liu, Bruce G. Szczepankiewicz, Zhonghua Pei, David A. Janowick, Zhili Xin, Philip J. Hajduk, Cele Abad-Zapatero, Heng Liang, Charles W. Hutchins, Stephen W. Fesik, Steve J. Ballaron, Mike A. Stashko, Tom Lubben, Amanda K. Mika, Bradley A. Zinker, James M. Trevillyan, and Michael R. Jirousek
pp 2093–2103Publication Date (Web): April 12, 2003 (Article)
DOI: 10.1021/jm0205696
Structure−Activity Relationships of Dynorphin A Analogues Modified in the Address Sequence
Georg Schlechtingen, Robert N. DeHaven, Jeffrey D. Daubert, Joel A. Cassel, Nga N. Chung, Peter W. Schiller, Joseph P. Taulane, and Murray Goodman
pp 2104–2109Publication Date (Web): April 19, 2003 (Article)
DOI: 10.1021/jm020125+
Full Text HTMLRational Design and Synthesis of an Orally Active Indolopyridone as a Novel Conformationally Constrained Cannabinoid Ligand Possessing Antiinflammatory Properties
Stephen T. Wrobleski, Ping Chen, John Hynes, Jr., Shuqun Lin, Derek J. Norris, Chennagiri R. Pandit, Steven Spergel, Hong Wu, John S. Tokarski, Xiaorong Chen, Kathleen M. Gillooly, Peter A. Kiener, Kim W. McIntyre, Vina Patil-koota, David J. Shuster, Lori A. Turk, Guchen Yang, and Katerina Leftheris
pp 2110–2116Publication Date (Web): April 26, 2003 (Article)
DOI: 10.1021/jm020329q
Synthesis of Chiral 1-[ω-(4-Chlorophenoxy)alkyl]-4-methylpiperidines and Their Biological Evaluation at σ1, σ2, and Sterol Δ8−Δ7 Isomerase Sites
Francesco Berardi, Fulvio Loiodice, Giuseppe Fracchiolla, Nicola Antonio Colabufo, Roberto Perrone, and Vincenzo Tortorella
pp 2117–2124Publication Date (Web): April 25, 2003 (Article)
DOI: 10.1021/jm021014d
Modulation of P-Glycoprotein-Mediated Multidrug Resistance by Flavonoid Derivatives and Analogues
Mohamed Hadjeri, Magali Barbier, Xavier Ronot, Anne-Marie Mariotte, Ahcène Boumendjel, and Jean Boutonnat
pp 2125–2131Publication Date (Web): April 19, 2003 (Article)
DOI: 10.1021/jm021099i
Unsymmetrical DNA Cross-Linking Agents: Combination of the CBI and PBD Pharmacophores
Moana Tercel, Stephen M. Stribbling, Hilary Sheppard, Bronwyn G. Siim, Kent Wu, Susan M. Pullen, K. Jane Botting, William R. Wilson, and William A. Denny
pp 2132–2151Publication Date (Web): April 25, 2003 (Article)
DOI: 10.1021/jm020526p
Discovery of a Simple Picomolar Inhibitor of Cholesteryl Ester Transfer Protein
Emily J. Reinhard, Jane L. Wang, Richard C. Durley, Yvette M. Fobian, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, Michele A. Promo, Michael B. Tollefson, William F. Vernier, Daniel T. Connolly, Bryan J. Witherbee, Michele A. Melton, Karen J. Regina, Mark E. Smith, and James A. Sikorski
pp 2152–2168Publication Date (Web): April 26, 2003 (Article)
DOI: 10.1021/jm020528+
Imidazoline Binding Sites (IBS) Profile Modulation: Key Role of the Bridge in Determining I1-IBS or I2-IBS Selectivity within a Series of 2-Phenoxymethylimidazoline Analogues
Francesco Gentili, Pascal Bousquet, Livio Brasili, Monique Dontenwill, Josiane Feldman, Francesca Ghelfi, Mario Giannella, Alessandro Piergentili, Wilma Quaglia, and Maria Pigini
pp 2169–2176Publication Date (Web): April 19, 2003 (Article)
DOI: 10.1021/jm021113r
Metal Coordination-Based Inhibitors of Adenylyl Cyclase: Novel Potent P-Site Antagonists
Daniel E. Levy, Ming Bao, Diana B. Cherbavaz, James E. Tomlinson, David M. Sedlock, Charles J. Homcy, and Robert M. Scarborough
pp 2177–2186Publication Date (Web): April 19, 2003 (Article)
DOI: 10.1021/jm0205604
Carbonic Anhydrase Inhibitors. Inhibition of Tumor-Associated Isozyme IX by Halogenosulfanilamide and Halogenophenylaminobenzolamide Derivatives
Marc A. Ilies, Daniela Vullo, Jaromir Pastorek, Andrea Scozzafava, Monica Ilies, Miron T. Caproiu, Silvia Pastorekova, and Claudiu T. Supuran
pp 2187–2196Publication Date (Web): April 19, 2003 (Article)
DOI: 10.1021/jm021123s
Carbonic Anhydrase Inhibitors. Inhibition of Cytosolic Isozymes I and II and Transmembrane, Tumor-Associated Isozyme IX with Sulfamates Including EMATE Also Acting as Steroid Sulfatase Inhibitors
Jean-Yves Winum, Daniela Vullo, Angela Casini, Jean-Louis Montero, Andrea Scozzafava, and Claudiu T. Supuran
pp 2197–2204Publication Date (Web): April 19, 2003 (Article)
DOI: 10.1021/jm021124k
Interaction of cis-(6-Benzhydrylpiperidin-3-yl)benzylamine Analogues with Monoamine Transporters: Structure−Activity Relationship Study of Structurally Constrained 3,6-Disubstituted Piperidine Analogues of (2,2-Diphenylethyl)-[1-(4-fluorobenzyl)piperidin-4-ylmethyl]amine
Rohit B. Kolhatkar, Sujit K. Ghorai, Clifford George, Maarten E. A. Reith, and Aloke K. Dutta
pp 2205–2215Publication Date (Web): April 19, 2003 (Article)
DOI: 10.1021/jm020561w
C(8) Substituted 1-Azabicyclo[3.3.1]non-3-enes and C(8) Substituted 1-Azabicyclo[3.3.1]nonan-4-ones: Novel Muscarinic Receptor Antagonists
Myoung Goo Kim, Erik T. Bodor, Chen Wang, T. Kendall Harden, and Harold Kohn
pp 2216–2226Publication Date (Web): April 26, 2003 (Article)
DOI: 10.1021/jm020572p
Identification of a Novel, Selective GABAA α5 Receptor Inverse Agonist Which Enhances Cognition
Mark S. Chambers, John R. Atack, Howard B. Broughton, Neil Collinson, Susan Cook, Gerard R. Dawson, Sarah C. Hobbs, George Marshall, Karen A. Maubach, Goplan V. Pillai, Austin J. Reeve, and Angus M. MacLeod
pp 2227–2240Publication Date (Web): April 25, 2003 (Article)
DOI: 10.1021/jm020582q
Determination of Conformer-Specific Partition Coefficients in Octanol/Water Systems
Márta Kraszni, István Bányai, and Béla Noszál
pp 2241–2245Publication Date (Web): April 30, 2003 (Article)
DOI: 10.1021/jm030767c
Brief Articles
Design, Synthesis, and Pharmacology of a Highly Subtype-Selective GluR1/2 Agonist, (RS)-2-Amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionic Acid (Cl-HIBO)
Esben J. Bjerrum, Anders S. Kristensen, Darryl S. Pickering, Jeremy R. Greenwood, Birgitte Nielsen, Tommy Liljefors, Arne Schousboe, Hans Bräuner-Osborne, and Ulf Madsen
pp 2246–2249Publication Date (Web): April 04, 2003 (Brief Article)
DOI: 10.1021/jm020588f
Distorting Malaria Peptide Backbone Structure to Enable Fitting into MHC Class II Molecules Renders Modified Peptides Immunogenic and Protective
Gladys Cifuentes, Manuel Elkin Patarroyo, Mauricio Urquiza, Luis E. Ramirez, Claudia Reyes, and Raul Rodriguez
pp 2250–2253Publication Date (Web): April 22, 2003 (Brief Article)
DOI: 10.1021/jm020440w
Nitro and Amino Substitution in the D-Ring of 5-(2-Dimethylaminoethyl)- 2,3-methylenedioxy-5H-dibenzo[c,h][1,6]naphthyridin-6-ones: Effect on Topoisomerase-I Targeting Activity and Cytotoxicity
Sudhir K. Singh, Alexander L. Ruchelman, Tsai-Kun Li, Angela Liu, Leroy F. Liu, and Edmond J. LaVoie
pp 2254–2257Publication Date (Web): April 09, 2003 (Article)
DOI: 10.1021/jm020498a
Book Reviews
Bioinformatics. From Genomes to Drugs Edited by Thomas Lengauer. Wiley-VCH, Weinheim, Germany. 2002. xx + 442 pp (first volume). xx + 206 pp (second volume). 17 × 24.5 cm. ISBN 3-527-29988-2. $265.00.
Donald B. Boyd
pp 2258–2259Publication Date (Web): April 23, 2003 (Book Review)
DOI: 10.1021/jm0301179
Free Energy Calculations in Rational Drug Design Edited by M. Rami Reddy and Mark D. Erion. Kluwer Academic/Plenum Publishers, New York. 2001. xxiii + 384 pp. 17 × 25.5 cm. ISBN 0-306-46667-7. $110.00
pp 2259–2260Publication Date (Web): April 19, 2003 (Book Review)
DOI: 10.1021/jm030151n