Table of Contents
December 29, 2005
Volume 48, Issue 26
Pages 8103-8298
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).
Letters
Semirational Design of (North)-Methanocarba Nucleosides as Dual Acting A1 and A3 Adenosine Receptor Agonists: Novel Prototypes for Cardioprotection
Kenneth A. Jacobson, Zhan-Guo Gao, Susanna Tchilibon, Heng T. Duong, Bhalchandra V. Joshi, Dmitry Sonin, and Bruce T. Liang
pp 8103–8107Publication Date (Web): November 24, 2005 (Letter)
DOI: 10.1021/jm050726b
Hi-Res PDFHuman P2Y6 Receptor: Molecular Modeling Leads to the Rational Design of a Novel Agonist Based on a Unique Conformational Preference
Stefano Costanzi, Bhalchandra V. Joshi, Savitri Maddileti, Liaman Mamedova, Maria J. Gonzalez-Moa, Victor E. Marquez, T. Kendall Harden, and Kenneth A. Jacobson
pp 8108–8111Publication Date (Web): November 23, 2005 (Letter)
DOI: 10.1021/jm050911p
Conversion of the Potent δ-Opioid Agonist H-Dmt-Tic-NH-CH2-Bid into δ-Opioid Antagonists by N1-Benzimidazole Alkylation1
Gianfranco Balboni, Remo Guerrini, Severo Salvadori, Lucia Negri, Elisa Giannini, Sharon D. Bryant, Yunden Jinsmaa, and Lawrence H. Lazarus
pp 8112–8114Publication Date (Web): November 23, 2005 (Letter)
DOI: 10.1021/jm058259l
Articles
Design, Synthesis, and Evaluation of Pharmacological Properties of Cinnamic Derivatives as Antiatherogenic Agents
Caroline Lapeyre, Mélanie Delomenède, Florence Bedos-Belval, Hubert Duran, Anne Nègre-Salvayre, and Michel Baltas
pp 8115–8124Publication Date (Web): November 11, 2005 (Article)
DOI: 10.1021/jm050454c
Charge Dependence of Cellular Uptake and Selective Antitumor Activity of Porphyrazines
Neal D. Hammer, Sangwan Lee, Benjamin J. Vesper, Kim M. Elseth, Brian M. Hoffman, Anthony G. M. Barrett, and James A. Radosevich
pp 8125–8133Publication Date (Web): November 12, 2005 (Article)
DOI: 10.1021/jm050466y
Estradiol−Adenosine Hybrid Compounds Designed to Inhibit Type 1 17β-Hydroxysteroid Dehydrogenase
Donald Poirier, Roch P. Boivin, Martin R. Tremblay, Marie Bérubé, Wei Qiu, and Sheng-Xiang Lin
pp 8134–8147Publication Date (Web): November 18, 2005 (Article)
DOI: 10.1021/jm058235e
Binding of Rasagiline-Related Inhibitors to Human Monoamine Oxidases: A Kinetic and Crystallographic Analysis
Claudia Binda, Frantisek Hubálek, Min Li, Yaacov Herzig, Jeffrey Sterling, Dale E. Edmondson, and Andrea Mattevi
pp 8148–8154Publication Date (Web): November 10, 2005 (Article)
DOI: 10.1021/jm0506266
Induced Fit in Mouse Acetylcholinesterase upon Binding a Femtomolar Inhibitor: A Molecular Dynamics Study
Sanjib Senapati, Jennifer M. Bui, and J. Andrew McCammon
pp 8155–8162Publication Date (Web): November 22, 2005 (Article)
DOI: 10.1021/jm050669m
(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: Platelet-Derived Growth Factor Receptor Tyrosine Kinase Inhibitors with Broad Antiproliferative Activity against Tumor Cells
Chih Y. Ho, Donald W. Ludovici, Umar S. M. Maharoof, Jay Mei, Jan L. Sechler, Robert W. Tuman, Eric D. Strobel, Laura Andraka, Hwa-Kwo Yen, Gregory Leo, Jian Li, Harold Almond, Hong Lu, Ann DeVine, Rose M. Tominovich, Judith Baker, Stuart Emanuel, Robert H. Gruninger, Steven A. Middleton, Dana L. Johnson, and Robert A. Galemmo, Jr.
pp 8163–8173Publication Date (Web): November 22, 2005 (Article)
DOI: 10.1021/jm050680m
Kynurenamines as Neural Nitric Oxide Synthase Inhibitors
Antonio Entrena, M. Encarnación Camacho, M. Dora Carrión, Luisa C. López-Cara, Guillermo Velasco, Josefa León, Germaine Escames, Darío Acuña-Castroviejo, Víctor Tapias, Miguel A. Gallo, Antonio Vivó, and Antonio Espinosa
pp 8174–8181Publication Date (Web): November 19, 2005 (Article)
DOI: 10.1021/jm050740o
N-Substituted cis-4a-(3-Hydroxyphenyl)-8a-methyloctahydroisoquinolines Are Opioid Receptor Pure Antagonists
F. Ivy Carroll, Sachin Chaudhari, James B. Thomas, S. Wayne Mascarella, Kenneth M. Gigstad, Jeffrey Deschamps, and Hernán A. Navarro
pp 8182–8193Publication Date (Web): November 16, 2005 (Article)
DOI: 10.1021/jm058261c
Novel Indole-Based Peroxisome Proliferator-Activated Receptor Agonists: Design, SAR, Structural Biology, and Biological Activities
Neeraj Mahindroo, Chien-Fu Huang, Yi-Huei Peng, Chiung-Chiu Wang, Chun-Chen Liao, Tzu-Wen Lien, Santhosh Kumar Chittimalla, Wei-Jan Huang, Chia-Hua Chai, Ekambaranellore Prakash, Ching-Ping Chen, Tsu-An Hsu, Cheng-Hung Peng, I-Lin Lu, Ling-Hui Lee, Yi-Wei Chang, Wei-Cheng Chen, Yu-Chen Chou, Chiung-Tong Chen, Chandra M. V. Goparaju, Yuan-Shou Chen, Shih-Jung Lan, Ming-Chen Yu, Xin Chen, Yu-Sheng Chao, Su-Ying Wu, and Hsing-Pang Hsieh
pp 8194–8208Publication Date (Web): November 18, 2005 (Article)
DOI: 10.1021/jm0506930
A New Bisintercalating Anthracycline with Picomolar DNA Binding Affinity
José Portugal, Derek J. Cashman, John O. Trent, Neus Ferrer-Miralles, Teresa Przewloka, Izabela Fokt, Waldemar Priebe, and Jonathan B. Chaires
pp 8209–8219Publication Date (Web): November 15, 2005 (Article)
DOI: 10.1021/jm050902g
Comparison of the NO and HNO Donating Properties of Diazeniumdiolates: Primary Amine Adducts Release HNO in Vivo
Katrina M. Miranda, Tatsuo Katori, Claudia L. Torres de Holding, Lynta Thomas, Lisa A. Ridnour, William J. McLendon, Stephanie M. Cologna, Andrew S. Dutton, Hunter C. Champion, Daniele Mancardi, Carlo G. Tocchetti, Joseph E. Saavedra, Larry K. Keefer, K. N. Houk, Jon M. Fukuto, David A. Kass, Nazareno Paolocci, and David A. Wink
pp 8220–8228Publication Date (Web): December 06, 2005 (Article)
DOI: 10.1021/jm050151i
Synthesis, Biological Activity, and Preliminary Pharmacokinetic Evaluation of Analogues of a Phosphosulfomannan Angiogenesis Inhibitor (PI-88)
Tomislav Karoli, Ligong Liu, Jon K. Fairweather, Edward Hammond, Cai Ping Li, Siska Cochran, Kicki Bergefall, Edward Trybala, Russell S. Addison, and Vito Ferro
pp 8229–8236Publication Date (Web): November 17, 2005 (Article)
DOI: 10.1021/jm050618p
Methyl Substitution on the Piperidine Ring of N-[ω-(6-Methoxynaphthalen-1-yl)alkyl] Derivatives as a Probe for Selective Binding and Activity at the σ1 Receptor
Francesco Berardi, Savina Ferorelli, Carmen Abate, Maria P. Pedone, Nicola A. Colabufo, Marialessandra Contino, and Roberto Perrone
pp 8237–8244Publication Date (Web): December 02, 2005 (Article)
DOI: 10.1021/jm050654o
New Potential Anticancer Agents Based on the Anthranilic Acid Scaffold. Synthesis and Evaluation of Biological Activity
Cenzo Congiu, Maria Teresa Cocco, Valentina Lilliu, and Valentina Onnis
pp 8245–8252Publication Date (Web): November 15, 2005 (Article)
DOI: 10.1021/jm050711d
2-(Benzimidazol-2-yl)quinoxalines: A Novel Class of Selective Antagonists at Human A1 and A3 Adenosine Receptors Designed by 3D Database Searching
Ettore Novellino, Barbara Cosimelli, Marina Ehlardo, Giovanni Greco, Manuela Iadanza, Antonio Lavecchia, Maria Grazia Rimoli, Annalisa Sala, Antonio Da Settimo, Giampaolo Primofiore, Federico Da Settimo, Sabrina Taliani, Concettina La Motta, Karl-Norbert Klotz, Daniela Tuscano, Maria Letizia Trincavelli, and Claudia Martini
pp 8253–8260Publication Date (Web): November 11, 2005 (Article)
DOI: 10.1021/jm050792d
Synthesis and Evaluation of Cyclic Secondary Amine Substituted Phenyl and Benzyl Nitrofuranyl Amides as Novel Antituberculosis Agents
Rajendra P. Tangallapally, Raghunandan Yendapally, Robin E. Lee, Anne J. M. Lenaerts, and Richard E. Lee
pp 8261–8269Publication Date (Web): November 17, 2005 (Article)
DOI: 10.1021/jm050765n
Synthesis of Tricyclic 1,3-Oxazin-4-ones and Kinetic Analysis of Cholesterol Esterase and Acetylcholinesterase Inhibition
Markus Pietsch and Michael Gütschow
pp 8270–8288Publication Date (Web): November 12, 2005 (Article)
DOI: 10.1021/jm0508639
Preparation and Biological Evaluation of Indole, Benzimidazole, and Thienopyrrole Piperazine Carboxamides: Potent Human Histamine H4 Antagonists
Jennifer D. Venable, Hui Cai, Wenying Chai, Curt A. Dvorak, Cheryl A. Grice, Jill A. Jablonowski, Chandra R. Shah, Annette K. Kwok, Kiev S. Ly, Barbara Pio, Jianmei Wei, Pragnya J. Desai, Wen Jiang, Steven Nguyen, Ping Ling, Sandy J. Wilson, Paul J. Dunford, Robin L. Thurmond, Timothy W. Lovenberg, Lars Karlsson, Nicholas I. Carruthers, and James P. Edwards
pp 8289–8298Publication Date (Web): November 23, 2005 (Article)
DOI: 10.1021/jm0502081