Journal of Medicinal Chemistry
Volume 43, Issue 22 (November 2, 2000)
Copyright © 2000 American Chemical Society

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COMMUNICATIONS

4041-4044

Discovery of Potent Cyclic Pseudopeptide Human Tachykinin NK-2 Receptor Antagonists Danilo Giannotti, Enzo Perrotta, Cristina Di Bugno, Rossano Nannicini, Nicholas J. S. Harmat, Alessandro Giolitti, Riccardo Patacchini, Anna Rita Renzetti, Luigi Rotondaro, Sandro Giuliani, Maria Altamura, and Carlo A. Maggi [Full Article - PDF]

EXPEDITED ARTICLES

4045-4050

(-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a Conformationally Restricted Analogue of Acetylcholine, Is a Highly Selective Full Agonist at the 7 Nicotinic Acetylcholine Receptor George Mullen, James Napier, Michael Balestra, Thomas DeCory, Gregory Hale, John Macor, Robert Mack, James Loch III, Ed Wu, Alexander Kover, Patrick Verhoest, Anthony Sampognaro, Eifion Phillips, Yanyi Zhu, Robert Murray, Ronald Griffith, James Blosser, David Gurley, Anthony Machulskis, John Zongrone, Alan Rosen, and Jack Gordon [Full Article - PDF]

ARTICLES

4051-4062

Synthesis of Phenalene and Acenaphthene Derivatives as New Conformationally Restricted Ligands for Melatonin Receptors Carole Jellimann, Monique Mathé-Allainmat, Jean Andrieux, Stéphane Kloubert, Jean A. Boutin, Jean-Paul Nicolas, Caroline Bennejean, Philippe Delagrange, and Michel Langlois [Full Article - PDF]

4063-4070

Rational Design, Synthesis, and Biological Activity of Benzoxazinones as Novel Factor Xa Inhibitors Danette A. Dudley, Amy M. Bunker, Liguo Chi, Wayne L. Cody, Debra R. Holland, Diane P. Ignasiak, Nancy Janiczek-Dolphin, Thomas B. McClanahan, Thomas E. Mertz, Lakshmi S. Narasimhan, Stephen T. Rapundalo, Julia A. Trautschold, Chad A. Van Huis, and Jeremy J. Edmunds [Full Article - PDF]

4071-4083

Resistance-Modifying Agents. 8. Inhibition of O6-Alkylguanine-DNA Alkyltransferase by O6-Alkenyl-, O6-Cycloalkenyl-, and O6-(2-Oxoalkyl)guanines and Potentiation of Temozolomide Cytotoxicity in Vitro by O6-(1-Cyclopentenylmethyl)guanine Roger J. Griffin, Christine E. Arris, Christine Bleasdale, F. Thomas Boyle, A. Hilary Calvert, Nicola J. Curtin, Christine Dalby, Sreenivas Kanugula, Nicola K. Lembicz, David R. Newell, Anthony E. Pegg, and Bernard T. Golding [Full Article - PDF]

4084-4097

Resistance-Modifying Agents. 9. Synthesis and Biological Properties of Benzimidazole Inhibitors of the DNA Repair Enzyme Poly(ADP-ribose) Polymerase Alex W. White, Robert Almassy, A. Hilary Calvert, Nicola J. Curtin, Roger J. Griffin, Zdenek Hostomsky, Karen Maegley, David R. Newell, Sheila Srinivasan, and Bernard T. Golding [Full Article - PDF]

4098-4108

3D-QSAR CoMFA on Cyclin-Dependent Kinase Inhibitors Pierre Ducrot, Michel Legraverend, and David S. Grierson [Full Article - PDF]

4109-4117

Active Site Binding Modes of HIV-1 Integrase Inhibitors Christoph A. Sotriffer, Haihong Ni, and J. Andrew McCammon [Full Article - PDF]

4118-4125

Conformationally Constrained Anesthetic Steroids That Modulate GABAA Receptors Alison Anderson, Andrew C. Boyd, John K. Clark, Lee Fielding, David K. Gemmell, Niall M. Hamilton, Maurice S. Maidment, Valerie May, Ross McGuire, Petula McPhail, Francis H. Sansbury, Hardy Sundaram, and Robert Taylor [Full Article - PDF]

4126-4134

Thio- and Oxoflavopiridols, Cyclin-Dependent Kinase 1-Selective Inhibitors: Synthesis and Biological Effects Kyoung Soon Kim, John S. Sack, John S. Tokarski, Ligang Qian, Sam T. Chao, Leslie Leith, Yolanda F. Kelly, Raj N. Misra, John T. Hunt, S. David Kimball, William G. Humphreys, Barris S. Wautlet, Janet G. Mulheron, and Kevin R. Webster [Full Article - PDF]

4135-4150

Adenosine Analogues as Inhibitors of Trypanosoma brucei Phosphoglycerate Kinase: Elucidation of a Novel Binding Mode for a 2-Amino-N6-Substituted Adenosine Jerome C. Bressi, Jungwoo Choe, Melinda T. Hough, Frederick S. Buckner, Wesley C. Van Voorhis, Christophe L. M. J. Verlinde, Wim G. J. Hol, and Michael H. Gelb [Full Article - PDF]

4151-4159

2D QSAR Modeling and Preliminary Database Searching for Dopamine Transporter Inhibitors Using Genetic Algorithm Variable Selection of Molconn Z Descriptors Brian T. Hoffman, Theresa Kopajtic, Jonathan L. Katz, and Amy Hauck Newman [Full Article - PDF]

4160-4168

Sulfoxide-Containing Aromatic Nitrogen Mustards as Hypoxia-Directed Bioreductive Cytotoxins Zhong-Yue Sun, Emad Botros, Ai-Duen Su, Yu Kim, Enju Wang, Nesrine Z. Baturay, and Chul-Hoon Kwon [Full Article - PDF]

4169-4179

The Mitochondrial Monoamine Oxidase-Aldehyde Dehydrogenase Pathway: A Potential Site of Action of Daidzin Nadège Rooke, Dian-Jun Li, Junqing Li, and Wing Ming Keung [Full Article - PDF]

4180-4188

Calculation and Prediction of Binding Free Energies for the Matrix Metalloproteinases Oreola A. T. Donini and Peter A. Kollman [Full Article - PDF]

4189-4199

Synthesis and Biological Evaluation of Ceramide Analogues with Substituted Aromatic Rings or an Allylic Fluoride in the Sphingoid Moiety Ilse Van Overmeire, Swetlana A. Boldin, Krishnan Venkataraman, Rivka Zisling, Steven De Jonghe, Serge Van Calenbergh, Denis De Keukeleire, Anthony H. Futerman, and Piet Herdewijn [Full Article - PDF]

4200-4211

3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and Related 2-Urea Derivatives Are Potent and Selective Inhibitors of the FGF Receptor-1 Tyrosine Kinase Andrew M. Thompson, Cleo J. C. Connolly, James M. Hamby, Stacey Boushelle, Brian G. Hartl, Aneesa M. Amar, Alan J. Kraker, Denise L. Driscoll, Randall W. Steinkampf, Sandra J. Patmore, Patrick W. Vincent, Bill J. Roberts, William L. Elliott, Wayne Klohs, Wilbur R. Leopold, H. D. Hollis Showalter, and William A. Denny [Full Article - PDF]

4212-4218

Inhibition of Protein Synthesis by Didemnins: Cell Potency and SAR Deepika Ahuja, Adam Geiger, Joshi M. Ramanjulu, Matthew D. Vera, Bhagyashri SirDeshpande, Amy Pfizenmayer, Mohamed Abazeed, Daniel J. Krosky, David Beidler, Madeleine M. Joullié, and Peter L. Toogood [Full Article - PDF]

4219-4227

Novel Bronchodilators: Synthesis, Transamination Reactions, and Pharmacology of a Series of Pyrazino[2,3-c][1,2,6]thiadiazine 2,2-Dioxides Nuria Campillo, Concepción García, Pilar Goya, Ibon Alkorta, and Juan A. Páez [Full Article - PDF]

4228-4232

Syntheses and Antimalarial Activities of 10-Substituted Deoxoartemisinins Jingyuan Ma, Esther Katz, Dennis E. Kyle, and Herman Ziffer [Full Article - PDF]

4233-4246

Synthetic Oleanane and Ursane Triterpenoids with Modified Rings A and C: A Series of Highly Active Inhibitors of Nitric Oxide Production in Mouse Macrophages Tadashi Honda, BarbieAnn V. Rounds, Lothar Bore, Heather J. Finlay, Frank G. Favaloro, Jr., Nanjoo Suh, Yongping Wang, Michael B. Sporn, and Gordon W. Gribble [Full Article - PDF]

4247-4265

Synthesis, Biological Evaluation, and Conformational Analysis of A-Ring Diastereomers of 2-Methyl-1,25-dihydroxyvitamin D3 and Their 20-Epimers: Unique Activity Profiles Depending on the Stereochemistry of the A-Ring and at C-20 Katsuhiro Konno, Toshie Fujishima, Shojiro Maki, Zhaopeng Liu, Daishiro Miura, Manabu Chokki, Seiichi Ishizuka, Kentaro Yamaguchi, Yukiko Kan, Masaaki Kurihara, Naoki Miyata, Connie Smith, Hector F. DeLuca, and Hiroaki Takayama [Full Article - PDF]

4266-4277

Synthesis and Evaluation of Novel Steroidal Oxime Inhibitors of P450 17 (17-Hydroxylase/C17-20-Lyase) and 5-Reductase Types 1 and 2 Rolf W. Hartmann, Markus Hector, Samer Haidar, Peter B. Ehmer, Wolfgang Reichert, and Joachim Jose [Full Article - PDF]

4278-4287

Contribution of the Adenine Base to the Activity of Adenophostin A Investigated Using a Base Replacement Strategy Rachel D. Marwood, David J. Jenkins, Vanessa Correa, Colin W. Taylor, and Barry V. L. Potter [Full Article - PDF]

4288-4312

Structure-Activity Relationships of a Series of Pyrrolo[3,2-d]pyrimidine Derivatives and Related Compounds as Neuropeptide Y5 Receptor Antagonists Mark H. Norman, Ning Chen, Zhidong Chen, Christopher Fotsch, Clarence Hale, Nianhe Han, Ray Hurt, Tracy Jenkins, John Kincaid, Longbin Liu, Yuelie Lu, Ofir Moreno, Vincent J. Santora, Jennifer D. Sonnenberg, and William Karbon [Full Article - PDF]

4313-4318

Synthesis and Biological Activity of Novel 5-Fluoro-2'-deoxyuridine Phosphoramidate Prodrugs Caren L. Freel Meyers, Liping Hong, Carolyn Joswig, and Richard F. Borch [Full Article - PDF]

4319-4327

Activation Mechanisms of Nucleoside Phosphoramidate Prodrugs Caren L. Freel Meyers and Richard F. Borch [Full Article - PDF]

BRIEF ARTICLES

4328-4331

Hydrolytic Stability versus Ring Size in Lactams: Implications for the Development of Lactam Antibiotics and Other Serine Protease Inhibitors Peter Imming, Bernhard Klar, and Dorothea Dix [Full Article - PDF]

BOOK REVIEWS

4332-4332

Chromatography: Methods and Protocols. Volume 147, Methods in Molecular Biology Edited by Pascal Bailon, George K. Ehrlich, Wen-Jian Fung, and Wolfgang Berthold. Humana Press, Totowa, NJ. 2000. x + 230 pp. 15.5 × 23.5 cm. ISBN 0-89603-694-4. $79.50. Greg T. Hermanson [Full Article - PDF]