Table of Contents
March 11, 2004
Volume 47, Issue 6
Pages 1303-1594
About the Cover: Molecular modeling of overlayed trisubstituted acridine derivatives (mauve and green) complexed with G-quadruplex DNA (Harrison, R. J.; et al. J. Med. Chem. 2003, 46, 4463-4476).
Perspective
Selective Optimization of Side Activities: Another Way for Drug Discovery
Camille G. Wermuth
pp 1303–1314Publication Date (Web): February 13, 2004 (Perspective)
DOI: 10.1021/jm030480f
Hi-Res PDF Letters
A Non-Peptide NK1 Receptor Agonist Showing Subpicomolar Affinity
Andrea Cappelli, Germano Giuliani, Gal.la Pericot Mohr, Andrea Gallelli, Maurizio Anzini, Salvatore Vomero, Aroldo Cupello, Simona Scarrone, Mario Matarrese, Rosa Maria Moresco, Ferruccio Fazio, Federica Finetti, Lucia Morbidelli, and Marina Ziche
pp 1315–1318Publication Date (Web): February 11, 2004 (Letter)
DOI: 10.1021/jm034219a
Evaluation of Potent and Selective Small-Molecule Antagonists for the CXCR2 Chemokine Receptor
Katherine L. Widdowson, John D. Elliott, Daniel F. Veber, Hong Nie, Melvin C. Rutledge, Brent W. McCleland, Jia-Ning Xiang, Anthony J. Jurewicz, Robert P. Hertzberg, James J. Foley, Don E. Griswold, Lenox Martin, Judithann M. Lee, John R. White, and Henry M. Sarau
pp 1319–1321Publication Date (Web): February 11, 2004 (Letter)
DOI: 10.1021/jm034248l
Synthesis of a Potent Transition-State Inhibitor of 5‘-Deoxy-5‘-methylthioadenosine Phosphorylase
Vivekanand P. Kamath, Sandya Ananth, Shanta Bantia, and Philip E. Morris, Jr.
pp 1322–1324Publication Date (Web): February 17, 2004 (Letter)
DOI: 10.1021/jm030455+
Full Text HTMLCrystal Structures of Staphylococcus aureus Methionine Aminopeptidase Complexed with Keto Heterocycle and Aminoketone Inhibitors Reveal the Formation of a Tetrahedral Intermediate
Alice Douangamath, Glenn E. Dale, Allan D'Arcy, Michael Almstetter, Robert Eckl, Annabelle Frutos-Hoener, Bernd Henkel, Katrin Illgen, Sven Nerdinger, Henk Schulz, Aengus MacSweeney, Michael Thormann, Andreas Treml, Sabine Pierau, Sjoerd Wadman, and Christian Oefner
pp 1325–1328Publication Date (Web): February 07, 2004 (Letter)
DOI: 10.1021/jm034188j
Articles
Studies on Pyrrolopyrimidines as Selective Inhibitors of Multidrug-Resistance- Associated Protein in Multidrug Resistance
Shouming Wang, Adrian Folkes, Irina Chuckowree, Xiaoling Cockcroft, Sukhjit Sohal, Warren Miller, John Milton, Stephen P. Wren, Nigel Vicker, Paul Depledge, John Scott, Lyndsay Smith, Hazel Jones, Prakash Mistry, Richard Faint, Deanne Thompson, and Simon Cocks
pp 1329–1338Publication Date (Web): February 07, 2004 (Article)
DOI: 10.1021/jm031011g
Design and Synthesis of New Templates Derived from Pyrrolopyrimidine as Selective Multidrug-Resistance-Associated Protein Inhibitors in Multidrug Resistance
Shouming Wang, Nan Chi Wan, John Harrison, Warren Miller, Irina Chuckowree, Sukhjit Sohal, Timothy C. Hancox, Stewart Baker, Adrian Folkes, Francis Wilson, Deanne Thompson, Simon Cocks, Hayley Farmer, Anthony Boyce, Caroline Freathy, Jan Broadbridge, John Scott, Paul Depledge, Richard Faint, Prakash Mistry, and Peter Charlton
pp 1339–1350Publication Date (Web): February 07, 2004 (Article)
DOI: 10.1021/jm0310129
3-(4-Aroyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides as a New Class of Synthetic Histone Deacetylase Inhibitors. 3. Discovery of Novel Lead Compounds through Structure-Based Drug Design and Docking Studies,
Rino Ragno, Antonello Mai, Silvio Massa, Ilaria Cerbara, Sergio Valente, Patrizia Bottoni, Roberto Scatena, Florian Jesacher, Peter Loidl, and Gerald Brosch
pp 1351–1359Publication Date (Web): February 10, 2004 (Article)
DOI: 10.1021/jm031036f
A Computational Model for Anthracycline Binding to DNA: Tuning Groove-Binding Intercalators for Specific Sequences
Derek J. Cashman and Glen E. Kellogg
pp 1360–1374Publication Date (Web): February 14, 2004 (Article)
DOI: 10.1021/jm030529h
Structure-Based Optimization of Novel Azepane Derivatives as PKB Inhibitors
Christine B. Breitenlechner, Thomas Wegge, Laurent Berillon, Klaus Graul, Klaus Marzenell, Walter-Gunar Friebe, Ulrike Thomas, Ralf Schumacher, Robert Huber, Richard A. Engh, and Birgit Masjost
pp 1375–1390Publication Date (Web): February 17, 2004 (Article)
DOI: 10.1021/jm0310479
New Analogues of Amonafide and Elinafide, Containing Aromatic Heterocycles: Synthesis, Antitumor Activity, Molecular Modeling, and DNA Binding Properties
Miguel F. Braña, Mónica Cacho, Mario A. García, Beatriz de Pascual-Teresa, Ana Ramos, M. Teresa Domínguez, José M. Pozuelo, Cristina Abradelo, María Fernanda Rey-Stolle, Mercedes Yuste, Mónica Báñez-Coronel, and Juan Carlos Lacal
pp 1391–1399Publication Date (Web): February 07, 2004 (Article)
DOI: 10.1021/jm0308850
Identification of Opioid Ligands Possessing Mixed μ Agonist/δ Antagonist Activity among Pyridomorphinans Derived from Naloxone, Oxymorphone, and Hydropmorphone
Subramaniam Ananthan, Naveen K. Khare, Surendra K. Saini, Lainne E. Seitz, Jeffrey L. Bartlett, Peg Davis, Christina M. Dersch, Frank Porreca, Richard B. Rothman, and Edward J. Bilsky
pp 1400–1412Publication Date (Web): February 10, 2004 (Article)
DOI: 10.1021/jm030311v
Synthesis and Evaluation of Dihydropyrroloquinolines That Selectively Antagonize P-Glycoprotein
Brian D. Lee, Zhanjiang Li, Kevin J. French, Yan Zhuang, Zuping Xia, and Charles D. Smith
pp 1413–1422Publication Date (Web): February 10, 2004 (Article)
DOI: 10.1021/jm0303204
Orally Active Antimalarials: Hydrolytically Stable Derivatives of 10-Trifluoromethyl Anhydrodihydroartemisinin
Fabienne Grellepois, Fatima Chorki, Michèle Ourévitch, Sébastien Charneau, Philippe Grellier, Kylie A. McIntosh, William N. Charman, Bruno Pradines, Benoit Crousse, Danièle Bonnet-Delpon, and Jean-Pierre Bégué
pp 1423–1433Publication Date (Web): February 11, 2004 (Article)
DOI: 10.1021/jm030947m
Design, Synthesis, and Biological Evaluation of New 8-Heterocyclic Xanthine Derivatives as Highly Potent and Selective Human A2B Adenosine Receptor Antagonists
Pier Giovanni Baraldi, Mojgan Aghazadeh Tabrizi, Delia Preti, Andrea Bovero, Romeo Romagnoli, Francesca Fruttarolo, Naser Abdel Zaid, Allan R. Moorman, Katia Varani, Stefania Gessi, Stefania Merighi, and Pier Andrea Borea
pp 1434–1447Publication Date (Web): February 17, 2004 (Article)
DOI: 10.1021/jm0309654
Design, Synthesis, and Evaluation of Novel Thienopyrrolizinones as Antitubulin Agents
Vincent Lisowski, Stéphane Léonce, Laurence Kraus-Berthier, Jana Sopková-de Oliveira Santos, Alain Pierré, Ghanem Atassi, Daniel-Henri Caignard, Pierre Renard, and Sylvain Rault
pp 1448–1464Publication Date (Web): February 13, 2004 (Article)
DOI: 10.1021/jm030961z
Comparative in Vivo Stability of Copper-64-Labeled Cross-Bridged and Conventional Tetraazamacrocyclic Complexes
C. Andrew Boswell, Xiankai Sun, Weijun Niu, Gary R. Weisman, Edward H. Wong, Arnold L. Rheingold, and Carolyn J. Anderson
pp 1465–1474Publication Date (Web): February 12, 2004 (Article)
DOI: 10.1021/jm030383m
New 2,4-Diamino-5-(2‘,5‘-substituted benzyl)pyrimidines as Potential Drugs against Opportunistic Infections of AIDS and Other Immune Disorders. Synthesis and Species-Dependent Antifolate Activity
Andre Rosowsky, Ronald A. Forsch, Carol Hopkins Sibley, Clark B. Inderlied, and Sherry F. Queener
pp 1475–1486Publication Date (Web): February 05, 2004 (Article)
DOI: 10.1021/jm030438k
New Antibacterial Agents Derived from the DNA Gyrase Inhibitor Cyclothialidine
Peter Angehrn, Stefan Buchmann, Christoph Funk, Erwin Goetschi, Hans Gmuender, Paul Hebeisen, Dirk Kostrewa, Helmut Link, Thomas Luebbers, Raffaello Masciadri, Joergen Nielsen, Peter Reindl, Fabienne Ricklin, Anne Schmitt-Hoffmann, and Frank-Peter Theil
pp 1487–1513Publication Date (Web): February 05, 2004 (Article)
DOI: 10.1021/jm0310232
De Novo Design, Synthesis, and Pharmacology of α-Melanocyte Stimulating Hormone Analogues Derived from Somatostatin by a Hybrid Approach
Guoxia Han, Carrie Haskell-Luevano, Laura Kendall, Gregg Bonner, Mac E. Hadley, Roger D. Cone, and Victor J. Hruby
pp 1514–1526Publication Date (Web): February 07, 2004 (Article)
DOI: 10.1021/jm030452x
Anticonvulsant Activity of Phenylmethylenehydantoins: A Structure−Activity Relationship Study
Jeyanthi Chinnappa Thenmozhiyal, Peter Tsun-Hon Wong, and Wai-Keung Chui
pp 1527–1535Publication Date (Web): February 13, 2004 (Article)
DOI: 10.1021/jm030450c
First Reported Nonpeptide AT1 Receptor Agonist (L-162,313) Acts as an AT2 Receptor Agonist in Vivo
Yiqian Wan, Charlotta Wallinder, Berndt Johansson, Mathias Holm, Mahalingam A. K., Xiongyu Wu, Milad Botros, Anders Karlén, Anders Pettersson, Fred Nyberg, Lars Fändriks, Anders Hallberg, and Mathias Alterman
pp 1536–1546Publication Date (Web): February 14, 2004 (Article)
DOI: 10.1021/jm031031i
3-(4-Phenoxyphenyl)pyrazoles: A Novel Class of Sodium Channel Blockers
Ji Yang, Parviz Gharagozloo, Jiangchao Yao, Victor I. Ilyin, Richard B. Carter, Phong Nguyen, Silvia Robledo, Richard M. Woodward, and Derk J. Hogenkamp
pp 1547–1552Publication Date (Web): February 10, 2004 (Article)
DOI: 10.1021/jm030498q
Design, Synthesis, and Evaluation of Aza-Peptide Epoxides as Selective and Potent Inhibitors of Caspases-1, -3, -6, and -8
Karen Ellis James, Juliana L. Asgian, Zhao Zhao Li, Özlem Do
an Ekici, John R. Rubin, Jowita Mikolajczyk, Guy S. Salvesen, and James C. Powers
pp 1553–1574an Ekici, John R. Rubin, Jowita Mikolajczyk, Guy S. Salvesen, and James C. PowersPublication Date (Web): February 07, 2004 (Article)
DOI: 10.1021/jm0305016
Structure−Activity Relationships of Potent, Selective Inhibitors of Neuronal Nitric Oxide Synthase Based on the 6-Phenyl-2-aminopyridine Structure
John A. Lowe, III, Weimin Qian, Susan E. Drozda, Robert A. Volkmann, Deane Nason, Robert B. Nelson, Charles Nolan, Dane Liston, Karen Ward, Steve Faraci, Kim Verdries, Pat Seymour, Michael Majchrzak, Anabella Villalobos, and W. Frost White
pp 1575–1586Publication Date (Web): February 04, 2004 (Article)
DOI: 10.1021/jm030519g
Brief Articles
Arecoline Tripeptide Inhibitors of Proteasome
Mauro Marastoni, Anna Baldisserotto, Alessandro Canella, Riccardo Gavioli, Carmela De Risi, Gian Piero Pollini, and Roberto Tomatis
pp 1587–1590Publication Date (Web): February 10, 2004 (Brief Article)
DOI: 10.1021/jm0309102
New Steroidal Dimers with Antifungal and Antiproliferative Activity
Deepak B. Salunke, Braja G. Hazra, Vandana S. Pore, Manoj Kumar Bhat, Pallavi B. Nahar, and Mukund V. Deshpande
pp 1591–1594Publication Date (Web): February 11, 2004 (Brief Article)
DOI: 10.1021/jm030376y