Journal of Medicinal Chemistry
Volume 43, Issue 20 (October 5, 2000)
Copyright © 2000 American Chemical Society

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EXPEDITED ARTICLES

3587-3595

Discovery of (R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a Farnesyltransferase Inhibitor with Potent Preclinical Antitumor Activity John T. Hunt, Charles Z. Ding, Roberta Batorsky, Mark Bednarz, Rajeev Bhide, Young Cho, Saeho Chong, Sam Chao, Johnni Gullo-Brown, Peng Guo, Soong Hoon Kim, Francis Y. F. Lee, Katerina Leftheris, Arthur Miller, Toomas Mitt, Manorama Patel, Becky A. Penhallow, Carol Ricca, William C. Rose, Robert Schmidt, William A. Slusarchyk, Gregory Vite, and Veeraswamy Manne[Full Article - PDF]

ARTICLES

3596-3613

Synthesis and SAR of New 5-Phenyl-3-ureido-1,5-benzodiazepines as Cholecystokinin-B Receptor Antagonists Antonella Ursini, Anna M. Capelli, Robin A. E. Carr, Paolo Cassarà, Mauro Corsi, Ornella Curcuruto, Giovanni Curotto, Michele Dal Cin, Silvia Davalli, Daniele Donati, Aldo Feriani, Harry Finch, Gabriella Finizia, Giovanni Gaviraghi, Marc Marien, Giorgio Pentassuglia, Stefano Polinelli, Emiliangelo Ratti, Aldo Reggiani, Giorgio Tarzia, Giovanna Tedesco, Maria E. Tranquillini, David G. Trist, and Frank T. M. Van Amsterdam[Full Article - PDF]

3614-3623

Replacement of Glycine with Dicarbonyl and Related Moieties in Analogues of the C-Terminal Pentapeptide of Cholecystokinin: CCK2 Agonists Displaying a Novel Binding Mode Bruno Bellier, Marie-Emmanuelle Million, Sophie DaNascimento, Hervé Meudal, Safia Kellou, Bernard Maigret, and Christiane Garbay[Full Article - PDF]

3624-3631

Crystal Structure of FMN-Dependent Nitroreductase from Escherichia coli B: A Prodrug-Activating Enzyme Gary N. Parkinson, Jane V. Skelly, and Stephen Neidle[Full Article - PDF]

3632-3640

Design, Synthesis, and SAR of Novel Carbapenem Antibiotics with High Stability to Xanthomonas maltophilia Oxyiminocephalosporinase Type II Gholam H. Hakimelahi, Ali A. Moosavi-Movahedi, Shwu-Chen Tsay, Fu-Yuan Tsai, Jon D. Wright, Todor Dudev, Shahram Hakimelahi, and Carmay Lim[Full Article - PDF]

3641-3652

A Peptide Prodrug Approach for Improving Bisphosphonate Oral Absorption Aviva Ezra, Amnon Hoffman, Eli Breuer, Ivan S. Alferiev, Jukka Mönkkönen, Naama El Hanany-Rozen, Gal Weiss, David Stepensky, Irith Gati, Hagit Cohen, Soili Törmälehto, Gordon L. Amidon, and Gershon Golomb[Full Article - PDF]

3653-3664

New Substituted 1-(2,3-Dihydrobenzo[1,4]dioxin-2-ylmethyl)piperidin-4-yl Derivatives with 2-Adrenoceptor Antagonist Activity Patrice Mayer, Pascale Brunel, Céline Chaplain, Christel Piedecoq, Francis Calmel, Philippe Schambel, Philippe Chopin, Thierry Wurch, Petrus J. Pauwels, Marc Marien, Jean-Louis Vidaluc, and Thierry Imbert[Full Article - PDF]

3665-3670

Synthesis, Structure, and Antitumor Activity of a Novel Tetranuclear Titanium Complex Francesco Caruso, Miriam Rossi, Joseph Tanski, Rebeca Sartori, Renato Sariego, Sergio Moya, Sylvia Diez, Ema Navarrete, Augusto Cingolani, Fabio Marchetti, and Claudio Pettinari[Full Article - PDF]

3671-3676

Synthesis and Hypolipidemic and Antiplatelet Activities of -Asarone Isomers in Humans (in Vitro), Mice (in Vivo), and Rats (in Vivo) Janusz Popawski, Boena ozowicka, Alina T. Dubis, Barbara Lachowska, Stanisaw Witkowski, Danuta Siluk, Jacek Petrusewicz, Roman Kaliszan, Jacek Cybulski, Magorzata Strzakowska, and Zdzisaw Chilmonczyk[Full Article - PDF]

3677-3687

Carbonic Anhydrase and Matrix Metalloproteinase Inhibitors: Sulfonylated Amino Acid Hydroxamates with MMP Inhibitory Properties Act as Efficient Inhibitors of CA Isozymes I, II, and IV, and N-Hydroxysulfonamides Inhibit Both These Zinc Enzymes Andrea Scozzafava and Claudiu T. Supuran[Full Article - PDF]

3688-3698

Synthesis of New Indeno[1,2-c]isoquinolines: Cytotoxic Non-Camptothecin Topoisomerase I Inhibitors Mark Cushman, Muthusamy Jayaraman, Jeffrey A. Vroman, Anna K. Fukunaga, Brian M. Fox, Glenda Kohlhagen, Dirk Strumberg, and Yves Pommier[Full Article - PDF]

3699-3703

Deriving a Quantitative Chirality Measure from Molecular Similarity Indices Romualdo Benigni, Marina Cotta-Ramusino, Grazia Gallo, Fabrizio Giorgi, Alessandro Giuliani, and Maria Rosaria Varì[Full Article - PDF]

3704-3713

Synthesis and Cytotoxicity of 4-Amino-5-oxopyrido[2,3-d]pyrimidine Nucleosides Jean-Luc Girardet, Esmir Gunic, Cathey Esler, Dariusz Cieslak, Zbigniew Pietrzkowski, and Guangyi Wang[Full Article - PDF]

3714-3717

Fast Calculation of Molecular Polar Surface Area as a Sum of Fragment-Based Contributions and Its Application to the Prediction of Drug Transport Properties Peter Ertl, Bernhard Rohde, and Paul Selzer[Full Article - PDF]

3718-3735

Benzo[c]quinolizin-3-ones: A Novel Class of Potent and Selective Nonsteroidal Inhibitors of Human Steroid 5-Reductase 1 Antonio Guarna, Fabrizio Machetti, Ernesto G. Occhiato, and Dina Scarpi , Alessandra Comerci, Giovanna Danza, Rosa Mancina, and Mario Serio , Kimber Hardy[Full Article - PDF]

3736-3745

Nonpeptide v3 Antagonists. 1. Transformation of a Potent, Integrin-Selective IIb3 Antagonist into a Potent v3 Antagonist Mark E. Duggan, Le T. Duong, John E. Fisher, Terence G. Hamill, William F. Hoffman, Joel R. Huff, Nathan C. Ihle, Chih-Tai Leu, Rose M. Nagy, James J. Perkins, Sevgi B. Rodan, Gregg Wesolowski, David B. Whitman, Amy E. Zartman, Gideon A. Rodan, and George D. Hartman[Full Article - PDF]

3746-3751

Synthesis and Opioid Receptor Affinity of a Series of 2,4-Diaryl-Substituted 3,7-Diazabicylononanones Tom Siener, Antonella Cambareri, Ulrich Kuhl, Werner Englberger, Michael Haurand, Babette Kögel, and Ulrike Holzgrabe[Full Article - PDF]

3752-3760

Synthesis of Novel 3,7-Substituted-2-(3',4'-dihydroxyphenyl)flavones with Improved Antioxidant Activity Frédérique A. A. van Acker, Jos A. Hageman, Guido R. M. M. Haenen, Wim J. F. van der Vijgh, Aalt Bast, and Wiro M. P. B. Menge[Full Article - PDF]

3761-3769

New Arylpiperazine Derivatives as Antagonists of the Human Cloned 5-HT4 Receptor Isoforms Sophie Curtet, Jean-Louis Soulier, Ivan Zahradnik, Mireille Giner, Isabelle Berque-Bestel, Jeanne Mialet, Frank Lezoualc'h, Patrick Donzeau-Gouge, Sames Sicsic, Rodolphe Fischmeister, and Michel Langlois[Full Article - PDF]

3770-3777

-Turned Dipeptoids as Potent and Selective CCK1 Receptor Antagonists Mercedes Martín-Martínez, Natalia De la Figuera, Miriam Latorre, Rosario Herranz, M. Teresa García-López, Edurne Cenarruzabeitia, Joaquín Del Río, and Rosario González-Muñiz[Full Article - PDF]

3778-3785

Novel Cannabinol Probes for CB1 and CB2 Cannabinoid Receptors Anu Mahadevan, Craig Siegel, Billy R. Martin, Mary E. Abood, Irina Beletskaya, and Raj K. Razdan[Full Article - PDF]

3786-3791

Binding of a Diverse Set of Ligands to Avidin and Streptavidin: An Accurate Quantitative Prediction of Their Relative Affinities by a Combination of Molecular Mechanics and Continuum Solvent Models Bernd Kuhn and Peter A. Kollman[Full Article - PDF]

BRIEF ARTICLES

3792-3798

Synthesis of New 2,6-Prolylxylidide Analogues of Tocainide as Stereoselective Blockers of Voltage-Gated Na+ Channels with Increased Potency and Improved Use-Dependent Activity Carlo Franchini, Filomena Corbo, Giovanni Lentini, Gemma Bruno, Antonio Scilimati, Vincenzo Tortorella, Diana Conte Camerino, and Annamaria De Luca[Full Article - PDF]

3799-3802

6-Aminoquinolones as New Potential Anti-HIV Agents Violetta Cecchetti, Cristina Parolin, Stefano Moro, Teresa Pecere, Enrica Filipponi, Arianna Calistri, Oriana Tabarrini, Barbara Gatto, Manlio Palumbo, Arnaldo Fravolini, and Giorgio Palu'\t[Full Article - PDF]

3803-3808

Melanoma Peptide MART-1(27-35) Analogues with Enhanced Binding Capacity to the Human Class I Histocompatibility Molecule HLA-A2 by Introduction of a -Amino Acid Residue: Implications for Recognition by Tumor-Infiltrating Lymphocytes Gilles Guichard, Annette Zerbib, Frédérique-Anne Le Gal, Johan Hoebeke, Francine Connan, Jeannine Choppin, Jean-Paul Briand, and Jean-Gérard Guillet[Full Article - PDF]

3809-3812

Synthesis, Antibacterial, and Cytotoxic Evaluation of Certain 7-Substituted Norfloxacin Derivatives Kuo-Chang Fang, Yeh-Long Chen, Jia-Yuh Sheu, Tai-Chi Wang, and Cherng-Chyi Tzeng[Full Article - PDF]

BOOK REVIEWS

3813-3813

Platinum-Based Drugs in Cancer Therapy Edited by Lloyd R. Kendall and Nicholas P. Farrell. Humana Press, Totowa, NJ. 2000. xii + 341 pp. 16 × 23.5 cm. ISBN 0-896-03599-9. $145.00. J. A. Cowan [Full Article - PDF]

3813-3813

Traditional Chinese Medicine - Molecular Structures, Natural Sources, and Applications By X. Yan, J. Zhou, and G. Xie. Edited and with an introduction by G. W. A. Milne. Ashgate Publishing, Ltd., Hampshire, U.K. 1999. vii + 1024 pp. 17.5 ± 25 cm. ISBN 0 566 08210 1. $295.00. Kuo-Hsiung Lee [Full Article - PDF]

3814-3814

[Full Article - PDF]