Table of Contents
April 22, 2004
Volume 47, Issue 9
Pages 2171-2392
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).
Letters
Estrogen Receptor Ligands. II. Discovery of Benzoxathiins as Potent, Selective Estrogen Receptor α Modulators
Seongkon Kim, Jane Y. Wu, Elizabeth T. Birzin, Katalin Frisch, Wanda Chan, Lee-Yuh Pai, Yi Tien Yang, Ralph T. Mosley, Paula M. D. Fitzgerald, Nandini Sharma, Johanna Dahllund, Ann-Gerd Thorsell, Frank DiNinno, Susan P. Rohrer, James M. Schaeffer, and Milton L. Hammond
pp 2171–2175Publication Date (Web): March 20, 2004 (Letter)
DOI: 10.1021/jm034243o
Hi-Res PDFSelective, Orally Active γ-Aminobutyric AcidA α5 Receptor Inverse Agonists as Cognition Enhancers
Francine Sternfeld, Robert W. Carling, Richard A. Jelley, Tamara Ladduwahetty, Kevin J. Merchant, Kevin W. Moore, Austin J. Reeve, Leslie J. Street, Desmond O'Connor, Bindi Sohal, John R. Atack, Susan Cook, Guy Seabrook, Keith Wafford, F. David Tattersall, Neil Collinson, Gerard R. Dawson, José L. Castro, and Angus M. MacLeod
pp 2176–2179Publication Date (Web): March 27, 2004 (Letter)
DOI: 10.1021/jm031076j
Articles
Synthesis and Selective Cyclooxygenase-2 Inhibitory Activity of a Series of Novel, Nitric Oxide Donor-Containing Pyrazoles
Ramani R. Ranatunge, Michael Augustyniak, Upul K. Bandarage, Richard A. Earl, James L. Ellis, David S. Garvey, David R. Janero, L. Gordon Letts, Allison M. Martino, Madhavi G. Murty, Stewart K. Richardson, Joseph D. Schroeder, Matthew J. Shumway, S. William Tam, A. Mark Trocha, and Delano V. Young
pp 2180–2193Publication Date (Web): March 27, 2004 (Article)
DOI: 10.1021/jm030276s
Identification of Putative Agouti-Related Protein(87−132)-Melanocortin-4 Receptor Interactions by Homology Molecular Modeling and Validation Using Chimeric Peptide Ligands
Andrzej Wilczynski, Xiang S. Wang, Christine G. Joseph, Zhimin Xiang, Rayna M. Bauzo, Joseph W. Scott, Nicholas B. Sorensen, Amanda M. Shaw, William J. Millard, Nigel G. Richards, and Carrie Haskell-Luevano
pp 2194–2207Publication Date (Web): March 20, 2004 (Article)
DOI: 10.1021/jm0303608
Synthesis and Evaluation of Two 18F-Labeled 6-Iodo-2-(4‘-N,N-dimethylamino)phenylimidazo[1,2-a]pyridine Derivatives as Prospective Radioligands for β-Amyloid in Alzheimer's Disease
Lisheng Cai, Frederick T. Chin, Victor W. Pike, Hiroshi Toyama, Jeih-San Liow, Sami S. Zoghbi, Kendra Modell, Emmanuelle Briard, H. Umesha Shetty, Kathryn Sinclair, Sean Donohue, Dnyanesh Tipre, Mei-Ping Kung, Claudio Dagostin, David A. Widdowson, Michael Green, Weiyi Gao, Mary M. Herman, Masanori Ichise, and Robert B. Innis
pp 2208–2218Publication Date (Web): March 20, 2004 (Article)
DOI: 10.1021/jm030477w
Comparative Molecular Field Analysis and Comparative Molecular Similarity Indices Analysis of Thalidomide Analogues as Angiogenesis Inhibitors
Erin R. Lepper, Sylvia S. W. Ng, Michael Gütschow, Michael Weiss, Sunna Hauschildt, Thomas K. Hecker, Frederick A. Luzzio, Kurt Eger, and William D. Figg
pp 2219–2227Publication Date (Web): March 27, 2004 (Article)
DOI: 10.1021/jm0304820
Development of a New Radioligand, N-(5-Fluoro-2-phenoxyphenyl)-N-(2-[18F]fluoroethyl-5-methoxybenzyl)acetamide, for PET Imaging of Peripheral Benzodiazepine Receptor in Primate Brain
Ming-Rong Zhang, Jun Maeda, Masanao Ogawa, Junko Noguchi, Takehito Ito, Yuichiro Yoshida, Takashi Okauchi, Shigeru Obayashi, Tetsuya Suhara, and Kazutoshi Suzuki
pp 2228–2235Publication Date (Web): March 26, 2004 (Article)
DOI: 10.1021/jm0304919
Synthesis, Biological Activity, and Quantitative Structure−Activity Relationship Study of Azanaphthalimide and Arylnaphthalimide Derivatives
Miguel F. Braña, Ana Gradillas, Angel Gómez, Nuria Acero, Francisco Llinares, Dolores Muñoz-Mingarro, Cristina Abradelo, Fernanda Rey-Stolle, Mercedes Yuste, Joaquín Campos, Miguel Á. Gallo, and Antonio Espinosa
pp 2236–2242Publication Date (Web): March 20, 2004 (Article)
DOI: 10.1021/jm0310784
Novel Amino Acid Derived Natural Products from the Ascidian Atriolum robustum: Identification and Pharmacological Characterization of a Unique Adenosine Derivative
Stefan Kehraus, Simone Gorzalka, Christian Hallmen, Jamshed Iqbal, Christa E. Müller, Anthony D. Wright, Michael Wiese, and Gabriele M. König
pp 2243–2255Publication Date (Web): March 30, 2004 (Article)
DOI: 10.1021/jm031092g
Synthesis and Structure−Activity Relationship of Novel Antitumoral Platinum Xanthate Complexes
Wolfgang Friebolin, Gerhard Schilling, Margot Zöller, and Eberhard Amtmann
pp 2256–2263Publication Date (Web): March 20, 2004 (Article)
DOI: 10.1021/jm0309405
Heterocyclic Bis-Cations as Starting Hits for Design of Inhibitors of the Bifunctional Enzyme Histidine-Containing Protein Kinase/Phosphatase from Bacillus subtilis
Helena Ramström, Maryline Bourotte, Claude Philippe, Martine Schmitt, Jacques Haiech, and Jean-Jacques Bourguignon
pp 2264–2275Publication Date (Web): March 26, 2004 (Article)
DOI: 10.1021/jm021043o
Combination of Paclitaxel and Nitric Oxide as a Novel Treatment for the Reduction of Restenosis
Chia-En Lin, David S. Garvey, David R. Janero, L. Gordon Letts, Przemyslaw Marek, Stewart K. Richardson, Diana Serebryanik, Matthew J. Shumway, S. William Tam, A. Mark Trocha, and Delano V. Young
pp 2276–2282Publication Date (Web): March 26, 2004 (Article)
DOI: 10.1021/jm0304111
Structure−Activity Relationship of Purine Ribonucleosides for Inhibition of Hepatitis C Virus RNA-Dependent RNA Polymerase
Anne B. Eldrup, Charles R. Allerson, C. Frank Bennett, Sanjib Bera, Balkrishen Bhat, Neelima Bhat, Michele R. Bosserman, Jennifer Brooks, Christine Burlein, Steven S. Carroll, P. Dan Cook, Krista L. Getty, Malcolm MacCoss, Daniel R. McMasters, David B. Olsen, Thazha P. Prakash, Marija Prhavc, Quanlai Song, Joanne E. Tomassini, and Jie Xia
pp 2283–2295Publication Date (Web): March 26, 2004 (Article)
DOI: 10.1021/jm030424e
Bisguanidine, Bis(2-aminoimidazoline), and Polyamine Derivatives as Potent and Selective Chemotherapeutic Agents against Trypanosoma brucei rhodesiense. Synthesis and in Vitro Evaluation
Christophe Dardonville and Reto Brun
pp 2296–2307Publication Date (Web): March 26, 2004 (Article)
DOI: 10.1021/jm031024u
4-(Tetralin-1-yl)- and 4-(Naphthalen-1-yl)alkyl Derivatives of 1-Cyclohexylpiperazine as σ Receptor Ligands with Agonist σ2 Activity
Francesco Berardi, Savina Ferorelli, Carmen Abate, Nicola Antonio Colabufo, Marialessandra Contino, Roberto Perrone, and Vincenzo Tortorella
pp 2308–2317Publication Date (Web): March 30, 2004 (Article)
DOI: 10.1021/jm031026e
Design, Synthesis, and Biological Evaluation of Substituted 2-Cyclohexyl-4-phenyl-1H-imidazoles: Potent and Selective Neuropeptide Y Y5-Receptor Antagonists
Charles A. Blum, Xiaozhang Zheng, and Stéphane De Lombaert
pp 2318–2325Publication Date (Web): March 20, 2004 (Article)
DOI: 10.1021/jm030490g
Khellinone Derivatives as Blockers of the Voltage-Gated Potassium Channel Kv1.3: Synthesis and Immunosuppressive Activity
Jonathan B. Baell, Robert W. Gable, Andrew J. Harvey, Nathan Toovey, Tanja Herzog, Wolfram Hänsel, and Heike Wulff
pp 2326–2336Publication Date (Web): March 05, 2004 (Article)
DOI: 10.1021/jm030523s
Carbonic Anhydrase Inhibitors. Design of Selective, Membrane-Impermeant Inhibitors Targeting the Human Tumor-Associated Isozyme IX
Joseph. R. Casey, Patricio E. Morgan, Daniela Vullo, Andrea Scozzafava, Antonio Mastrolorenzo, and Claudiu T. Supuran
pp 2337–2347Publication Date (Web): March 20, 2004 (Article)
DOI: 10.1021/jm031079w
Dopamine D4 Ligands and Models of Receptor Activation: 2-(4-Pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and Related Heteroarylmethylarylpiperazines Exhibit a Substituent Effect Responsible for Additional Efficacy Tuning
Andrew O. Stewart, Marlon D. Cowart, Robert B. Moreland, Steve P. Latshaw, Mark A. Matulenko, Pramila A. Bhatia, Xueqing Wang, Jerome F. Daanen, Sherry L. Nelson, Marc A. Terranova, Marian T. Namovic, Diana L. Donnelly-Roberts, Loan N. Miller, Masaki Nakane, James P. Sullivan, and Jorge D. Brioni
pp 2348–2355Publication Date (Web): March 23, 2004 (Article)
DOI: 10.1021/jm0305669
Application of Predictive QSAR Models to Database Mining: Identification and Experimental Validation of Novel Anticonvulsant Compounds
Min Shen, Cécile Béguin, Alexander Golbraikh, James P. Stables, Harold Kohn, and Alexander Tropsha
pp 2356–2364Publication Date (Web): March 20, 2004 (Article)
DOI: 10.1021/jm030584q
Synthesis and Biological Activity of Sulfonamide Derivatives of Epipodophyllotoxin
Dominique Guianvarc'h, Maria Duca, Chawki Boukarim, Laurence Kraus-Berthier, Stéphane Léonce, Alain Pierré, Bruno Pfeiffer, Pierre Renard, Paola B. Arimondo, Claude Monneret, and Daniel Dauzonne
pp 2365–2374Publication Date (Web): March 30, 2004 (Article)
DOI: 10.1021/jm031117b
Design of Potent and Selective Agonists for the Human Vasopressin V1b Receptor Based on Modifications of [Deamino-Cys1]arginine Vasopressin at Position 4
Ling Ling Cheng, Stoytcho Stoev, Maurice Manning, Sylvain Derick, Ana Pena, Mohamed Ben Mimoun, and Gilles Guillon
pp 2375–2388Publication Date (Web): March 30, 2004 (Article)
DOI: 10.1021/jm030611c
Brief Articles
Structural and Energetic Analyses of the Effects of the K103N Mutation of HIV-1 Reverse Transcriptase on Efavirenz Analogues
Marina Udier-Blagović, Julian Tirado-Rives, and William L. Jorgensen
pp 2389–2392Publication Date (Web): March 20, 2004 (Brief Article)
DOI: 10.1021/jm0303507