Table of Contents
January 27, 2005
Volume 48, Issue 2
Pages 337-654
About the Cover: Interaction of the β-L-enantiomer of a 4'-C-ethynyl-2',3'-dideoxynucleoside analogue (ent-14-TP) at the active site of HIV reverse transcriptase (Siddiqui, M. A.; et al. J. Med. Chem. 2004, 47, 5041-5048).
From Diatomics to Drugs and Distributions
W. Graham Richards
pp 337–344Publication Date (Web): December 10, 2004 (Perspective)
DOI: 10.1021/jm040136y
Hi-Res PDF Letters
Studies toward the Pharmacophore of Salvinorin A, a Potent κ Opioid Receptor Agonist
Thomas A. Munro, Mark A. Rizzacasa, Bryan L. Roth, Beth A. Toth, and Feng Yan
pp 345–348Publication Date (Web): December 29, 2004 (Letter)
DOI: 10.1021/jm049438q
Generation of “Neoheparin” from E. coli K5 Capsular Polysaccharide
Ulf Lindahl, Jin-ping Li, Marion Kusche-Gullberg, Markku Salmivirta, Sakari Alaranta, Timo Veromaa, Jef Emeis, Ian Roberts, Clare Taylor, Pasqua Oreste, Giorgio Zoppetti, Annamaria Naggi, Giangiacomo Torri, and Benito Casu
pp 349–352Publication Date (Web): December 31, 2004 (Letter)
DOI: 10.1021/jm049812m
Discovery of 5-Arylsulfonamido-3- (pyrrolidin-2-ylmethyl)-1H-indole Derivatives as Potent, Selective 5-HT6 Receptor Agonists and Antagonists
Derek C. Cole, William J. Lennox, Sabrina Lombardi, John W. Ellingboe, Ronald C. Bernotas, Gregory J. Tawa, Hossein Mazandarani, Deborah L. Smith, Guoming Zhang, Joseph Coupet, and Lee E. Schechter
pp 353–356Publication Date (Web): December 21, 2004 (Letter)
DOI: 10.1021/jm049243i
Synthesis, Characterization, and Plasma Lipoprotein Association of a Nucleus-Targeted Boronated Porphyrin
Paola Dozzo, Myoung-Seo Koo, Stephanie Berger, Trudy M. Forte, and Stephen B. Kahl
pp 357–359Publication Date (Web): December 30, 2004 (Letter)
DOI: 10.1021/jm049277q
Rational Approach To Discover Multipotent Anti-Alzheimer Drugs
Michela Rosini, Vincenza Andrisano, Manuela Bartolini, Maria L. Bolognesi, Patrizia Hrelia, Anna Minarini, Andrea Tarozzi, and Carlo Melchiorre
pp 360–363Publication Date (Web): December 31, 2004 (Letter)
DOI: 10.1021/jm049112h
Articles
Selective Estrogen Receptor Modulators with Conformationally Restricted Side Chains. Synthesis and Structure−Activity Relationship of ERα-Selective Tetrahydroisoquinoline Ligands
Johanne Renaud, Serge François Bischoff, Thomas Buhl, Philipp Floersheim, Brigitte Fournier, Martin Geiser, Christine Halleux, Joerg Kallen, Hansjoerg Keller, and Paul Ramage
pp 364–379Publication Date (Web): December 22, 2004 (Article)
DOI: 10.1021/jm040858p
Stereoselective Synthesis of [l-Arg-l/d-3-(2-naphthyl)alanine]-Type (E)-Alkene Dipeptide Isosteres and Its Application to the Synthesis and Biological Evaluation of Pseudopeptide Analogues of the CXCR4 Antagonist FC131
Hirokazu Tamamura, Kenichi Hiramatsu, Satoshi Ueda, Zixuan Wang, Shuichi Kusano, Shigemi Terakubo, John O. Trent, Stephen C. Peiper, Naoki Yamamoto, Hideki Nakashima, Akira Otaka, and Nobutaka Fujii
pp 380–391Publication Date (Web): December 21, 2004 (Article)
DOI: 10.1021/jm049429h
Aminoimidazolylmethyluracil Analogues as Potent Inhibitors of Thymidine Phosphorylase and Their Bioreductive Nitroimidazolyl Prodrugs
Philip Reigan, Philip N. Edwards, Abdul Gbaj, Christian Cole, Simon T. Barry, Ken M. Page, Susan E. Ashton, Richard W. A. Luke, Kenneth T. Douglas, Ian J. Stratford, Mohammed Jaffar, Richard A. Bryce, and Sally Freeman
pp 392–402Publication Date (Web): December 24, 2004 (Article)
DOI: 10.1021/jm049494r
Fragment-Based Lead Discovery Using X-ray Crystallography
Michael J. Hartshorn, Christopher W. Murray, Anne Cleasby, Martyn Frederickson, Ian J. Tickle, and Harren Jhoti
pp 403–413Publication Date (Web): December 21, 2004 (Article)
DOI: 10.1021/jm0495778
Identification of Novel p38α MAP Kinase Inhibitors Using Fragment-Based Lead Generation
Adrian L. Gill, Martyn Frederickson, Anne Cleasby, Steven J. Woodhead, Maria G. Carr, Andrew J. Woodhead, Margaret T. Walker, Miles S. Congreve, Lindsay A. Devine, Dominic Tisi, Marc O'Reilly, Lisa C. A. Seavers, Deborah J. Davis, Jayne Curry, Rachel Anthony, Alessandro Padova, Christopher W. Murray, Robin A. E. Carr, and Harren Jhoti
pp 414–426Publication Date (Web): December 21, 2004 (Article)
DOI: 10.1021/jm049575n
Potent 4-Aryl- or 4-Arylalkyl-Substituted 3-Isoxazolol GABAA Antagonists: Synthesis, Pharmacology, and Molecular Modeling
Bente Frølund, Lars S. Jensen, Luca Guandalini, Carolina Canillo, Henrik T. Vestergaard, Uffe Kristiansen, Birgitte Nielsen, Tine B. Stensbøl, Christian Madsen, Povl Krogsgaard-Larsen, and Tommy Liljefors
pp 427–439Publication Date (Web): December 22, 2004 (Article)
DOI: 10.1021/jm049256w
Quantitative Structure−Activity Relationship Analysis of Inhibitors of the Nicotine Metabolizing CYP2A6 Enzyme
Minna Rahnasto, Hannu Raunio, Antti Poso, Carsten Wittekindt, and Risto O. Juvonen
pp 440–449Publication Date (Web): December 24, 2004 (Article)
DOI: 10.1021/jm049536b
Synthesis and Antiviral Evaluation of Cis-Substituted Cyclohexenyl and Cyclohexanyl Nucleosides
Karine Barral, Jérôme Courcambeck, Gérard Pèpe, Jan Balzarini, Johan Neyts, Erik De Clercq, and Michel Camplo
pp 450–456Publication Date (Web): December 23, 2004 (Article)
DOI: 10.1021/jm0493966
Quantitative Structure−Activity Relationship (5D-QSAR) Study of Combretastatin-like Analogues as Inhibitors of Tubulin Assembly
Sylvie Ducki, Grant Mackenzie, Nicholas J. Lawrence, and James P. Snyder
pp 457–465Publication Date (Web): December 31, 2004 (Article)
DOI: 10.1021/jm049444m
Investigations on the Effects of Basic Side Chains on the Hormonal Profile of (4R,5S)/(4S,5R)-4,5-Bis(4-hydroxyphenyl)-2-imidazolines
Moriz von Rauch, Sandra Busch, and Ronald Gust
pp 466–474Publication Date (Web): December 18, 2004 (Article)
DOI: 10.1021/jm040855c
The Novel l- and d-Amino Acid Derivatives of Hydroxyurea and Hydantoins: Synthesis, X-ray Crystal Structure Study, and Cytostatic and Antiviral Activity Evaluations
Ninoslav Opačić, Monika Barbarić, Branka Zorc, Mario Cetina, Ante Nagl, Danijel Frković, Marijeta Kralj, Krešimir Pavelić, Jan Balzarini, Graciela Andrei, Robert Snoeck, Erik De Clercq, Silvana Raić-Malić, and Mladen Mintas
pp 475–482Publication Date (Web): December 31, 2004 (Article)
DOI: 10.1021/jm040869i
Endothelin-Converting Enzyme-1 Inhibition and Growth of Human Glioblastoma Cells
Yann Berger, Henrietta Dehmlow, Denise Blum-Kaelin, Eric A. Kitas, Bernd-Michael Löffler, Johannes D. Aebi, and Lucienne Juillerat-Jeanneret
pp 483–498Publication Date (Web): December 31, 2004 (Article)
DOI: 10.1021/jm040857x
Identification of 4-Substituted 1,2,3-Triazoles as Novel Oxazolidinone Antibacterial Agents with Reduced Activity against Monoamine Oxidase A
Folkert Reck, Fei Zhou, Marc Girardot, Gunther Kern, Charles J. Eyermann, Neil J. Hales, Rona R. Ramsay, and Michael B. Gravestock
pp 499–506Publication Date (Web): January 04, 2005 (Article)
DOI: 10.1021/jm0400810
Somatostatin Receptor 1 Selective Analogues: 2. Nα-Methylated Scan
Judit Erchegyi, Carl A. Hoeger, William Low, Daniel Hoyer, Beatrice Waser, Véronique Eltschinger, Jean-Claude Schaer, Renzo Cescato, Jean Claude Reubi, and Jean E. Rivier
pp 507–514Publication Date (Web): December 23, 2004 (Article)
DOI: 10.1021/jm049520l
Somatostatin Receptor 1 Selective Analogues: 3. Dicyclic Peptides
Jean E. Rivier, Dean A. Kirby, Judit Erchegyi, Beatrice Waser, Véronique Eltschinger, Renzo Cescato, and Jean Claude Reubi
pp 515–522Publication Date (Web): December 23, 2004 (Article)
DOI: 10.1021/jm049519m
Somatostatin Receptor 1 Selective Analogues: 4. Three-Dimensional Consensus Structure by NMR
Christy Rani R. Grace, Lukas Durrer, Steven C. Koerber, Judit Erchegyi, Jean Claude Reubi, Jean E. Rivier, and Roland Riek
pp 523–533Publication Date (Web): December 23, 2004 (Article)
DOI: 10.1021/jm049518u
Synthesis and Antiviral Activity of Helioxanthin Analogues
Hosup Yeo, Ying Li, Lei Fu, Ju-Liang Zhu, Elizabeth A. Gullen, Ginger E. Dutschman, Yashang Lee, Raymond Chung, Eng-Shang Huang, David J. Austin, and Yung-Chi Cheng
pp 534–546Publication Date (Web): December 23, 2004 (Article)
DOI: 10.1021/jm034265a
Sulfonamide Drugs Binding to the Colchicine Site of Tubulin: Thermodynamic Analysis of the Drug−Tubulin Interactions by Isothermal Titration Calorimetry
Mithu Banerjee, Asim Poddar, Gopa Mitra, Avadhesha Surolia, Takashi Owa, and Bhabatarak Bhattacharyya
pp 547–555Publication Date (Web): December 21, 2004 (Article)
DOI: 10.1021/jm0494974
Further Naphthylcombretastatins. An Investigation on the Role of the Naphthalene Moiety
Ana B. S. Maya, Concepción Pérez-Melero, Carmen Mateo, Dulce Alonso, José Luis Fernández, Consuelo Gajate, Faustino Mollinedo, Rafael Peláez, Esther Caballero, and Manuel Medarde
pp 556–568Publication Date (Web): December 31, 2004 (Article)
DOI: 10.1021/jm0310737
Selective Benzopyranone and Pyrimido[2,1-a]isoquinolin-4-one Inhibitors of DNA-Dependent Protein Kinase: Synthesis, Structure−Activity Studies, and Radiosensitization of a Human Tumor Cell Line in Vitro
Roger J. Griffin, Gabriele Fontana, Bernard T. Golding, Sophie Guiard, Ian R. Hardcastle, Justin J. J. Leahy, Niall Martin, Caroline Richardson, Laurent Rigoreau, Martin Stockley, and Graeme C. M. Smith
pp 569–585Publication Date (Web): December 29, 2004 (Article)
DOI: 10.1021/jm049526a
Development of Potent μ-Opioid Receptor Ligands Using Unique Tyrosine Analogues of Endomorphin-2
Tingyou Li, Yoshio Fujita, Yuko Tsuda, Anna Miyazaki, Akihiro Ambo, Yusuke Sasaki, Yunden Jinsmaa, Sharon D. Bryant, Lawrence H. Lazarus, and Yoshio Okada
pp 586–592Publication Date (Web): December 23, 2004 (Article)
DOI: 10.1021/jm049384k
Synthesis and Biological Study of a New Series of 4‘-Demethylepipodophyllotoxin Derivatives
Maria Duca, Dominique Guianvarc'h, Philippe Meresse, Emmanuel Bertounesque, Daniel Dauzonne, Laurence Kraus-Berthier, Sylvie Thirot, Stéphane Léonce, Alain Pierré, Bruno Pfeiffer, Pierre Renard, Paola B. Arimondo, and Claude Monneret
pp 593–603Publication Date (Web): December 31, 2004 (Article)
DOI: 10.1021/jm0495733
Exploring the Role of Different Drug Transport Routes in Permeability Screening
Pär Matsson, Christel A. S. Bergström, Naoki Nagahara, Staffan Tavelin, Ulf Norinder, and Per Artursson
pp 604–613Publication Date (Web): December 18, 2004 (Article)
DOI: 10.1021/jm049711o
4,6-Disubstituted 2,2-Dimethylchromans Structurally Related to the KATP Channel Opener Cromakalim: Design, Synthesis, and Effect on Insulin Release and Vascular Tone
Sophie Sebille, Pascal de Tullio, Bénédicte Becker, Marie-Hélène Antoine, Stéphane Boverie, Bernard Pirotte, and Philippe Lebrun
pp 614–621Publication Date (Web): December 18, 2004 (Article)
DOI: 10.1021/jm040789e
Antitumor-Active Cobalt−Alkyne Complexes Derived from Acetylsalicylic Acid: Studies on the Mode of Drug Action
Ingo Ott, Kathrin Schmidt, Brigitte Kircher, Petra Schumacher, Thomas Wiglenda, and Ronald Gust
pp 622–629Publication Date (Web): December 30, 2004 (Article)
DOI: 10.1021/jm049326z
Comparison of Trace Metal Concentrations in Malign and Benign Human Prostate
Mehmet Yaman, Demet Atici, Sezgin Bakırdere, and İsmail Akdeniz
pp 630–634Publication Date (Web): December 22, 2004 (Article)
DOI: 10.1021/jm0494568
Extension of the Nenitzescu Reaction to Simple Ketones Provides an Efficient Route to 1‘-Alkyl-5‘-hydroxynaltrindole Analogues, Potent and Selective δ-Opioid Receptor Antagonists
Shefali, Sanjay K. Srivastava, Stephen M. Husbands, and John W. Lewis
pp 635–638Publication Date (Web): December 31, 2004 (Article)
DOI: 10.1021/jm040853s
Quinols as Novel Therapeutic Agents. 2.1 4-(1-Arylsulfonylindol-2-yl)-4-hydroxycyclohexa-2,5-dien-1-ones and Related Agents as Potent and Selective Antitumor Agents
Jane M. Berry, Tracey D. Bradshaw, Iduna Fichtner, Ruobo Ren, Carl H. Schwalbe, Geoffrey Wells, Eng-Hui Chew, Malcolm F. G. Stevens, and Andrew D. Westwell
pp 639–644Publication Date (Web): December 23, 2004 (Article)
DOI: 10.1021/jm040859h
Synthesis and Enzyme-Specific Activation of Carbohydrate−Geldanamycin Conjugates with Potent Anticancer Activity
Hao Cheng, Xianhua Cao, Ming Xian, Lanyan Fang, Tingwei Bill Cai, Jacqueline Jia Ji, Josefino B. Tunac, Duxin Sun, and Peng George Wang
pp 645–652Publication Date (Web): December 31, 2004 (Article)
DOI: 10.1021/jm049693a
Book Reviews
Progress in Medicinal Chemistry. Volume 42 Edited by F. D. King, G. Lawton, and A. W. Oxford. Elsevier, Amsterdam, The Netherlands. 2004. x + 393 pp. 14.5 × 21.5 cm. ISBN 0444-51143-1. $209.00.
Robert K. Griffith
p 653Publication Date (Web): December 24, 2004 (Book Review)
DOI: 10.1021/jm040197w
Design and Synthesis of a Fluoroindolocarbazole Series as Selective Topoisomerase I Active Agents. Discovery of Water-Soluble 3,9-Difluoro-12,13-dihydro-13-[6-amino-β-d-glucopyranosyl]-5H,13H-benzo[b]thienyl[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione (BMS-251873) with Curative Antitumor Activity against Prostate Carcinoma Xenograft Tumor Model.
Balu N. Balasubramanian, Denis R. St. Laurent, Mark G. Saulnier, Byron H. Long, Carol Bachand, Francis Beaulieu, Wendy Clarke, Milind Deshpande, Jeffrey Eummer, Craig R. Fairchild, David B. Frennesson, Robert Kramer, Frank Y. Lee, Mikael Mahler, Alain Martel, B. Narasimhulu Naidu, William C. Rose, John Russell, Edward Ruediger, Carola Solomon, Karen M. Stoffan, Henry Wong, John J. Wright, Kurt Zimmermann, and Dolatrai M. Vyas:
p 654Publication Date (Web): December 29, 2004 (Addition/Correction)
DOI: 10.1021/jm040089+
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