Journal of Medicinal Chemistry
Volume 44, Issue 25 (December 6, 2001)
Copyright © 2001 American Chemical Society

Click  [Full Article - PDF] to display or print the full article page image in PDF. Note: As of August 2000, Acrobat Reader 4.0 or later is recommended for PDFs.

LETTERS

4309-4312

Conformationally Constrained Analogues of Diacylglycerol. 18. The Incorporation of a Hydroxamate Moiety into Diacylglycerol-Lactones Reduces Lipophilicity and Helps Discriminate between sn-1 and sn-2 Binding Modes to Protein Kinase C (PK-C). Implications for Isozyme Specificity Jeewoo Lee, Kee-Chung Han, Ji-Hye Kang, Larry L. Pearce, Nancy E. Lewin, Shunqi Yan, Samira Benzaria, Marc C. Nicklaus, Peter M. Blumberg, and Victor E. Marquez [Full Article - PDF]

ARTICLES

4313-4324

Discovery of Small-Molecule Inhibitors of Bcl-2 through Structure-Based Computer Screening Istvan J. Enyedy, Yan Ling, Kassoum Nacro, York Tomita, Xihan Wu, Yeyu Cao, Ribo Guo, Bihua Li, Xiaofeng Zhu, Ying Huang, Ya-Qiu Long, Peter P. Roller, Dajun Yang, and Shaomeng Wang [Full Article - PDF]

4325-4338

Free Energy Component Analysis for Drug Design: A Case Study of HIV-1 Protease-Inhibitor Binding Parul Kalra, T. Vasisht Reddy, and B. Jayaram [Full Article - PDF]

4339-4358

Oxindole-Based Inhibitors of Cyclin-Dependent Kinase 2 (CDK2): Design, Synthesis, Enzymatic Activities, and X-ray Crystallographic Analysis H. Neal Bramson, John Corona, Stephen T. Davis, Scott H. Dickerson, Mark Edelstein, Stephen V. Frye, Robert T. Gampe, Jr., Phil A. Harris, Anne Hassell, William D. Holmes, Robert N. Hunter, Karen E. Lackey, Brett Lovejoy, Michael J. Luzzio, Val Montana, Warren J. Rocque, David Rusnak, Lisa Shewchuk, James M. Veal, Duncan H. Walker, and Lee F. Kuyper [Full Article - PDF]

4359-4369

[1,2,4]Triazino[4,3-a]benzimidazole Acetic Acid Derivatives: A New Class of Selective Aldose Reductase Inhibitors Federico Da Settimo, Giampaolo Primofiore, Antonio Da Settimo, Concettina La Motta, Sabrina Taliani, Francesca Simorini, Ettore Novellino, Giovanni Greco, Antonio Lavecchia, and Enrico Boldrini [Full Article - PDF]

4370-4378

Cheminformatic Models To Predict Binding Affinities to Human Serum Albumin Gonzalo Colmenarejo, Ana Alvarez-Pedraglio, and José-Luis Lavandera [Full Article - PDF]

4379-4392

Systematic Structure-Based Design and Stereoselective Synthesis of Novel Multisubstituted Cyclopentane Derivatives with Potent Antiinfluenza Activity Pooran Chand, Pravin L. Kotian, Ali Dehghani, Yahya El-Kattan, Tsu-Hsing Lin, Tracy L. Hutchison, Y. Sudhakar Babu, Shanta Bantia, Arthur J. Elliott, and John A. Montgomery [Full Article - PDF]

4393-4403

Discovery of Novel p-Arylthio Cinnamides as Antagonists of Leukocyte Function-Associated Antigen-1/Intercellular Adhesion Molecule-1 Interaction. 4. Structure-Activity Relationship of Substituents on the Benzene Ring of the Cinnamide Martin Winn, Edward B. Reilly, Gang Liu, Jeffrey R. Huth, Hwan-Soo Jae, Jennifer Freeman, Zhonghua Pei, Zhili Xin, John Lynch, Jeff Kester, Thomas W. von Geldern, Sandra Leitza, Peter DeVries, Robert Dickinson, Donna Mussatto, and Gregory F. Okasinski [Full Article - PDF]

4404-4415

Synthesis and Structure-Activity Relationships of N-(1-Benzylpiperidin-4-yl)arylacetamide Analogues as Potent 1 Receptor Ligands Yunsheng Huang, Philip S. Hammond, Li Wu, and Robert H. Mach [Full Article - PDF]

4416-4430

New Antimitotic Agents with Activity in Multi-Drug-Resistant Cell Lines and in Vivo Efficacy in Murine Tumor Models Bruce G. Szczepankiewicz, Gang Liu, Hwan-Soo Jae, Andrew S. Tasker, Indrani W.Gunawardana, Thomas W. von Geldern, Stephen L. Gwaltney, II, J. Ruth Wu-Wong, Laura Gehrke, William J. Chiou, R. Bruce Credo, Jeffery D. Alder, Michael A. Nukkala, Nicolette A. Zielinski, Ken Jarvis, Karl W. Mollison, David J. Frost, Joy L. Bauch, Yu Hua Hui, Akiyo K. Claiborne, Qun Li, and Saul H. Rosenberg [Full Article - PDF]

4431-4442

trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: A New Class of Potent and Selective 5-HT1A Receptor Ligands as Conformationally Constrained Analogues of 4-[3-(5-Methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1- arylpiperazines Roberto Perrone, Francesco Berardi, Nicola A. Colabufo, Marcello Leopoldo, Enza Lacivita, and Vincenzo Tortorella , Amedeo Leonardi, Elena Poggesi, and Rodolfo Testa [Full Article - PDF]

4443-4452

Antimalarial Alkoxylated and Hydroxylated Chalones: Structure-Activity Relationship Analysis Mei Liu, Prapon Wilairat, and Mei-Lin Go [Full Article - PDF]

4453-4461

Novel Tropane-Based Irreversible Ligands for the Dopamine Transporter Mu-Fa Zou, Theresa Kopajtic, Jonathan L. Katz, Sara Wirtz, Joseph B. Justice, Jr., and Amy Hauck Newman [Full Article - PDF]

4462-4467

O-Phosphonatomethylcholine, Its Analogues, Alkyl Esters, and Their Biological Activity Antonín Hol, Berta Otová, Milo Budínsk, David Emerson, and Marc E. Wiles [Full Article - PDF]

4468-4474

3-(Arylacetylamino)-N-methylbenzamides: A Novel Class of Selective Anti-Helicobacter pylori Agents Ryoichi Ando, Makoto Kawamura, and Noriko Chiba [Full Article - PDF]

4475-4480

Synthesis and Biological Studies of Novel Nucleoside Phosphoramidate Prodrugs Sandra C. Tobias and Richard F. Borch [Full Article - PDF]

4481-4491

Nonsteroidal Selective Glucocorticoid Modulators: the Effect of C-5 Alkyl Substitution on the Transcriptional Activation/Repression Profile of 2,5-Dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines Steven W. Elmore, Michael J. Coghlan, David D. Anderson, John K. Pratt, Brian E. Green, Alan X. Wang, Michael A. Stashko, Chun W. Lin, Curtis M. Tyree, Jeffery N. Miner, Peer B. Jacobson, Denise M. Wilcox, and Benjamin C. Lane [Full Article - PDF]

BRIEF ARTICLES

4492-4496

Design, Synthesis, and Biological Activity of a Novel Non-Cisplatin-type Platinum-Acridine Pharmacophore Elizabeth T. Martins, Hemanta Baruah, Jaroslaw Kramarczyk, Gilda Saluta, Cynthia S. Day, Gregory L. Kucera, and Ulrich Bierbach [Full Article - PDF]