Table of Contents
September 22, 2005
Volume 48, Issue 19
Pages 6140-6168
About the Cover: Illustration of the binding mode of a biheteroaryl inhibitor to vascular endothelial growth factor receptor-2 (Kuo, G.-H.; et al. J. Med. Chem. 2005, 48, 1886-1900).
Miniperspective
Synthetic Retinoids: Recent Developments Concerning Structure and Clinical Utility
Hiroyuki Kagechika and Koichi Shudo
pp 5875–5883Publication Date (Web): August 26, 2005 (Perspective)
DOI: 10.1021/jm0581821
Hi-Res PDF Letters
Discovery of Potent Orally Active Thrombin Receptor (Protease Activated Receptor 1) Antagonists as Novel Antithrombotic Agents
Samuel Chackalamannil, Yan Xia, William J. Greenlee, Martin Clasby, Darìo Doller, Hsingan Tsai, Theodros Asberom, Michael Czarniecki, Ho-Sam Ahn, George Boykow, Carolyn Foster, Jacqueline Agans-Fantuzzi, Matthew Bryant, Janice Lau, and Madhu Chintala
pp 5884–5887Publication Date (Web): August 24, 2005 (Letter)
DOI: 10.1021/jm0502236
Discovery and Characterization of Aminopiperidinecoumarin Melanin Concentrating Hormone Receptor 1 Antagonists
Philip R. Kym, Rajesh Iyengar, Andrew J. Souers, John K. Lynch, Andrew S. Judd, Ju Gao, Jennifer Freeman, Mathew Mulhern, Gang Zhao, Anil Vasudevan, Dariusz Wodka, Christopher Blackburn, Jim Brown, Jennifer Lee Che, Courtney Cullis, Su Jen Lai, Matthew J. LaMarche, Tom Marsilje, Jon Roses, Todd Sells, Brad Geddes, Elizabeth Govek, Michael Patane, Dennis Fry, Brian D. Dayton, Sevan Brodjian, Doug Falls, Michael Brune, Eugene Bush, Robin Shapiro, Victoria Knourek-Segel, Thomas Fey, Cathleen McDowell, Glenn A. Reinhart, Lee C. Preusser, Kennan Marsh, Lisa Hernandez, Hing L. Sham, and Christine A. Collins
pp 5888–5891Publication Date (Web): August 19, 2005 (Letter)
DOI: 10.1021/jm050598r
Articles
Poly(amidoamine) Dendrimer-Based Multifunctional Engineered Nanodevice for Cancer Therapy
István J. Majoros, Thommey P. Thomas, Chandan B. Mehta, and James R. Baker Jr.
pp 5892–5899Publication Date (Web): August 26, 2005 (Article)
DOI: 10.1021/jm0401863
Discovery of the Novel Antithrombotic Agent 5-Chloro-N-({(5S)-2-oxo-3- [4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene- 2-carboxamide (BAY 59-7939): An Oral, Direct Factor Xa Inhibitor
Susanne Roehrig, Alexander Straub, Jens Pohlmann, Thomas Lampe, Josef Pernerstorfer, Karl-Heinz Schlemmer, Peter Reinemer, and Elisabeth Perzborn
pp 5900–5908Publication Date (Web): August 18, 2005 (Article)
DOI: 10.1021/jm050101d
4-Anilino-7,8-dialkoxybenzo[g]quinoline-3-carbonitriles as Potent Src Kinase Inhibitors
Dan M. Berger, Minu Dutia, Gary Birnberg, Dennis Powell, Diane H. Boschelli, Yanong D. Wang, Malini Ravi, Deanna Yaczko, Jennifer Golas, Judy Lucas, and Frank Boschelli
pp 5909–5920Publication Date (Web): August 25, 2005 (Article)
DOI: 10.1021/jm050512u
Development of Human Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonists. 1. Potent and Selective Small Molecule CGRP Antagonists. 1-[N2-[3,5-Dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1- piperidinyl]carbonyl]-d-tyrosyl]-l-lysyl]-4-(4-pyridinyl)piperazine: The First CGRP Antagonist for Clinical Trials in Acute Migraine
Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Helmut Pieper, Michael Entzeroth, Gerhard Hallermayer, and Henri Doods
pp 5921–5931Publication Date (Web): August 25, 2005 (Article)
DOI: 10.1021/jm0490641
Analogues of Thiolactomycin as Potential Antimalarial Agents
Simon M. Jones, Jonathan E. Urch, Marcel Kaiser, Reto Brun, John L. Harwood, Colin Berry, and Ian H. Gilbert
pp 5932–5941Publication Date (Web): August 30, 2005 (Article)
DOI: 10.1021/jm049067d
Deoxyuridine Triphosphate Nucleotidohydrolase as a Potential Antiparasitic Drug Target
Corinne Nguyen, Ganasan Kasinathan, Isabel Leal-Cortijo, Alexander Musso-Buendia, Marcel Kaiser, Reto Brun, Luis M. Ruiz-Pérez, Nils G. Johansson, Dolores González-Pacanowska, and Ian H. Gilbert
pp 5942–5954Publication Date (Web): August 19, 2005 (Article)
DOI: 10.1021/jm050111e
Imidazole-4,5-dicarboxamide Derivatives with Antiproliferative Activity against HL-60 Cells
Elisabeth M. Perchellet, Jean-Pierre Perchellet, and Paul W. Baures
pp 5955–5965Publication Date (Web): August 23, 2005 (Article)
DOI: 10.1021/jm050160r
Novel Inhibitor of p38 MAP Kinase as an Anti-TNF-α Drug: Discovery of N-[4-[2-Ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a Potent and Orally Active Anti-Rheumatoid Arthritis Agent
Seiji Miwatashi, Yasuyoshi Arikawa, Etsuo Kotani, Maki Miyamoto, Ken-ichi Naruo, Hiroyuki Kimura, Toshimasa Tanaka, Satoru Asahi, and Shigenori Ohkawa
pp 5966–5979Publication Date (Web): August 23, 2005 (Article)
DOI: 10.1021/jm050165o
F-18 Stilbenes as PET Imaging Agents for Detecting β-Amyloid Plaques in the Brain
Wei Zhang, Shunichi Oya, Mei-Ping Kung, Catherine Hou, Donna L. Maier, and Hank F. Kung
pp 5980–5988Publication Date (Web): August 23, 2005 (Article)
DOI: 10.1021/jm050166g
Differential Response of Estrogen Receptor Subtypes to 1,3-Diarylindene and 2,3-Diarylindene Ligands
Nicola J. Clegg, Sreenivasan Paruthiyil, Dale C. Leitman, and Thomas S. Scanlan
pp 5989–6003Publication Date (Web): August 19, 2005 (Article)
DOI: 10.1021/jm050226i
A New Pyridazine Series of GABAA α5 Ligands
Monique B. van Niel, Kevin Wilson, Charles H. Adkins, John R. Atack, José L. Castro, Dawn E. Clarke, Stephen Fletcher, Ute Gerhard, Mark M. Mackey, Sallie Malpas, Karen Maubach, Robert Newman, Desmond O'Connor, Gopalan V. Pillai, Peter B. Simpson, Steven R. Thomas, and Angus M. MacLeod
pp 6004–6011Publication Date (Web): August 23, 2005 (Article)
DOI: 10.1021/jm050249x
Fast Structure-Based Virtual Ligand Screening Combining FRED, DOCK, and Surflex
Maria A. Miteva, Wen H. Lee, Matthieu O. Montes, and Bruno O. Villoutreix
pp 6012–6022Publication Date (Web): August 30, 2005 (Article)
DOI: 10.1021/jm050262h
Conformationally Restricted Homotryptamines. 2. Indole Cyclopropylmethylamines as Selective Serotonin Reuptake Inhibitors
Ronald J. Mattson, John D. Catt, Derek J. Denhart, Jeffrey A. Deskus, Jonathan L. Ditta, Mendi A. Higgins, Lawrence R. Marcin, Charles P. Sloan, Brett R. Beno, Qi Gao, Melissa A. Cunningham, Gail K. Mattson, Thaddeus F. Molski, Matthew T. Taber, and Nicholas J. Lodge
pp 6023–6034Publication Date (Web): August 20, 2005 (Article)
DOI: 10.1021/jm0503291
Synthesis and in Vitro Evaluation of Inhibitors of Intestinal Cholesterol Absorption
Lisbet Kvrn, Moritz Werder, Helmut Hauser, and Erick M. Carreira
pp 6035–6053Publication Date (Web): August 25, 2005 (Article)
DOI: 10.1021/jm050422p
Rational Design, Synthesis, and Characterization of Novel Inhibitors for Human β1,4-Galactosyltransferase
Kenji Takaya, Noriko Nagahori, Masaki Kurogochi, Tetsuya Furuike, Nobuaki Miura, Kenji Monde, Yuan Chuan Lee, and Shin-Ichiro Nishimura
pp 6054–6065Publication Date (Web): August 27, 2005 (Article)
DOI: 10.1021/jm0504297
Thienopyrimidine Ureas as Novel and Potent Multitargeted Receptor Tyrosine Kinase Inhibitors
Yujia Dai, Yan Guo, Robin R. Frey, Zhiqin Ji, Michael L. Curtin, Asma A. Ahmed, Daniel H. Albert, Lee Arnold, Shannon S. Arries, Teresa Barlozzari, Joy L. Bauch, Jennifer J. Bouska, Peter F. Bousquet, George A. Cunha, Keith B. Glaser, Jun Guo, Junling Li, Patrick A. Marcotte, Kennan C. Marsh, Maria D. Moskey, Lori J. Pease, Kent D. Stewart, Vincent S. Stoll, Paul Tapang, Neil Wishart, Steven K. Davidsen, and Michael R. Michaelides
pp 6066–6083Publication Date (Web): August 26, 2005 (Article)
DOI: 10.1021/jm050458h
Molecular Modeling, Synthesis, and Preliminary Biological Evaluation of Glutathione-S-Transferase Inhibitors as Potential Therapeutic Agents
Antonio Procopio, Stefano Alcaro, Sante Cundari, Antonio De Nino, Francesco Ortuso, Paolo Sacchetta, Alfonso Pennelli, and Giovanni Sindona
pp 6084–6089Publication Date (Web): August 23, 2005 (Article)
DOI: 10.1021/jm0504609
Synthesis of Malarial Plasmepsin Inhibitors and Prediction of Binding Modes by Molecular Dynamics Simulations
Karolina Ersmark, Martin Nervall, Elizabeth Hamelink, Linda K. Janka, Jose C. Clemente, Ben M. Dunn, Michael J. Blackman, Bertil Samuelsson, Johan Åqvist, and Anders Hallberg
pp 6090–6106Publication Date (Web): August 23, 2005 (Article)
DOI: 10.1021/jm050463l
A Common Pharmacophore for a Diverse Set of Colchicine Site Inhibitors Using a Structure-Based Approach
Tam Luong Nguyen, Connor McGrath, Ann R. Hermone, James C. Burnett, Daniel W. Zaharevitz, Billy W. Day, Peter Wipf, Ernest Hamel, and Rick Gussio
pp 6107–6116Publication Date (Web): August 23, 2005 (Article)
DOI: 10.1021/jm050502t
Metabolic Regio- and Stereoselectivity of Cytochrome P450 2D6 towards 3,4-Methylenedioxy-N-alkylamphetamines: in Silico Predictions and Experimental Validation
Peter H. J. Keizers, Chris de Graaf, Frans J. J. de Kanter, Chris Oostenbrink, K. Anton Feenstra, Jan N. M. Commandeur, and Nico P. E. Vermeulen
pp 6117–6127Publication Date (Web): August 19, 2005 (Article)
DOI: 10.1021/jm050338+
Full Text HTMLBisphosphonate Inhibition of the Exopolyphosphatase Activity of the Trypanosoma brucei Soluble Vacuolar Pyrophosphatase
Evangelia Kotsikorou, Yongcheng Song, Julian M. W. Chan, Stephanie Faelens, Zev Tovian, Erin Broderick, Norbert Bakalara, Roberto Docampo, and Eric Oldfield
pp 6128–6139Publication Date (Web): August 25, 2005 (Article)
DOI: 10.1021/jm058220g
Synthesis, Anti-HIV Activity, and Metabolic Stability of New Alkenyldiarylmethane HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors
Bo-Liang Deng, Tracy L. Hartman, Robert W. Buckheit, Jr., Christophe Pannecouque, Erik De Clercq, Phillip E. Fanwick, and Mark Cushman
pp 6140–6155Publication Date (Web): July 23, 2008 (Article)
DOI: 10.1021/jm050452s
Synthesis and Evaluation of Neuroprotective α,β-Unsaturated Aldehyde Scavenger Histidyl-Containing Analogues of Carnosine
Andrea Guiotto, Andrea Calderan, Paolo Ruzza, Alessio Osler, Chiara Rubini, Dong-Gyu Jo, Mark P. Mattson, and Gianfranco Borin
pp 6156–6161Publication Date (Web): August 25, 2005 (Article)
DOI: 10.1021/jm050507q
Brief Articles
Thyrotropin-Releasing Hormone (TRH) Analogues That Exhibit Selectivity to TRH Receptor Subtype 2
Navneet Kaur, Xinping Lu, Marvin C. Gershengorn, and Rahul Jain
pp 6162–6165Publication Date (Web): August 19, 2005 (Brief Article)
DOI: 10.1021/jm0505462
Book Reviews
Natural Products. Drug Discovery and Therapeutic Medicine Edited by Lixin Zhang and Arnold L. Demain. Humana Press, Totowa, NJ. 2005. xiv + 384 pp. 18.5 × 26 cm. ISBN 1-58829-383-1. $135.00.
Kuo-Hsiung Lee
p 6166Publication Date (Web): August 6, 2005 (Book Review)
DOI: 10.1021/jm0582468
Frontiers in Medicinal Chemistry. Volume 2 Edited by Atta-ur-Rahman and Allen B. Reitz. Bentham Science Publishers, Ltd., Hilversum, The Netherlands. 2005. xii + 606 pp. ISBN 90-77527-01-X. $130.00.
Manfred E. Wolff
pp 6166–6167Publication Date (Web): August 5, 2005 (Book Review)
DOI: 10.1021/jm0582470
Name Reactions and Reagents in Organic Synthesis. Second Edition By Bradford P. Mundy, Michael G. Ellerd, and Frank G. Favaloro, Jr. Wiley-Interscience, Hoboken, NJ. 2005. xv + 882 pp. 16 × 24 cm. ISBN 0-471-22854-0. $89.95.
Kennerly S. Patrick
p 6166Publication Date (Web): August 20, 2005 (Book Review)
DOI: 10.1021/jm0582569
Organic Reaction Mechanisms. 2000 Edited by A. C. Knipe. John Wiley & Sons, Ltd., Chichester, West Sussex, England. 2004. ix + 667 pp. 15.5 × 23.5 cm. ISBN 0-470-85439-1. $565.00.
Wayne L. Cody
pp 6167–6168Publication Date (Web): August 20, 2005 (Book Review)
DOI: 10.1021/jm058254o
Chemoinformatics in Drug Discovery. Methods and Principles in Medicinal Chemistry. Volume 23 Edited by R. Mannhold, H. Kubinyi, and G. Folkers. Wiley-VCH Verlag GmbH, Weinheim, Germany. 2005. xxii + 493 pp. 17 × 25 cm. ISBN 3-5273-0753-2. $185.00.
Peter Gund
p 6168Publication Date (Web): August 25, 2005 (Book Review)
DOI: 10.1021/jm0582571