Journal of Medicinal Chemistry
Volume 42, Issue 19 (September 23, 1999)
Copyright © 1999 American Chemical Society

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PERSPECTIVES

3743-3778

Mixture-Based Synthetic Combinatorial Libraries Richard A. Houghten, Clemencia Pinilla, Jon R. Appel, Sylvie E. Blondelle, Colette T. Dooley, Jutta Eichler, Adel Nefzi, and John M. Ostresh [Full Article - PDF]

COMMUNICATIONS

3779-3784

N-Arylpiperazinone Inhibitors of Farnesyltransferase: Discovery and Biological Activity Theresa M. Williams, Jeffrey M. Bergman, Karen Brashear, Michael J. Breslin, Christopher J. Dinsmore, John H. Hutchinson, Suzanne C. MacTough, Craig A. Stump, Donna D. Wei, C. Blair Zartman, Michael J. Bogusky, J. Christopher Culberson, Carolyn Buser-Doepner, Joseph Davide, Ian B. Greenberg, Kelly A. Hamilton, Kenneth S. Koblan, Nancy E. Kohl, Dongming Liu, Robert B. Lobell, Scott D. Mosser, Timothy J. O'Neill, Elaine Rands, Michael D. Schaber, Francine Wilson, Edith Senderak, Sherri L. Motzel, Jackson B. Gibbs, Samuel L. Graham, David C. Heimbrook, George D. Hartman, Allen I. Oliff, and Joel R. Huff [Full Article - PDF]

3785-3788

A Ureido-Thioisobutyric Acid (GW9578) Is a Subtype-Selective PPAR Agonist with Potent Lipid-Lowering Activity Peter J. Brown, Deborah A. Winegar, Kelli D. Plunket, Linda B. Moore, Michael C. Lewis, Joan G. Wilson, Scott S. Sundseth, Cecilia S. Koble, Zhengdong Wu, James M. Chapman, Jürgen M. Lehmann, Steven A. Kliewer, and Timothy M. Willson [Full Article - PDF]

EXPEDITED ARTICLES

3789-3799

Discovery of Novel Antitumor Sulfonamides Targeting G1 Phase of the Cell Cycle Takashi Owa, Hiroshi Yoshino, Tatsuo Okauchi, Kentaro Yoshimatsu, Yoichi Ozawa, Naoko Hata Sugi, Takeshi Nagasu, Nozomu Koyanagi, and Kyosuke Kitoh [Full Article - PDF]

3800-3808

Novel Farnesol and Geranylgeraniol Analogues: A Potential New Class of Anticancer Agents Directed against Protein Prenylation Barbara S. Gibbs, Todd J. Zahn, YongQi Mu, Judith S. Sebolt-Leopold, and Richard A. Gibbs [Full Article - PDF]

ARTICLES

3809-3820

Design and Synthesis of Potent Non-Polyglutamatable Quinazoline Antifolate Thymidylate Synthase Inhibitors Peter R. Marsham, J. Michael Wardleworth, F. Thomas Boyle, Laurent F. Hennequin, Rosemary Kimbell, Melody Brown, and Ann L. Jackman [Full Article - PDF]

3821-3834

Occluded Molecular Surface Analysis of Ligand-Macromolecule Contacts: Application to HIV-1 Protease-Inhibitor Complexes Nagarajan Pattabiraman [Full Article - PDF]

3835-3844

Design and Fast Synthesis of C-Terminal Duplicated Potent C2-Symmetric P1/P1'-Modified HIV-1 Protease Inhibitors Mathias Alterman, Hans O. Andersson, Neeraj Garg, Göran Ahlsén, Seved Lövgren, Björn Classon, U. Helena Danielson, Ingmar Kvarnström, Lotta Vrang, Torsten Unge, Bertil Samuelsson, and Anders Hallberg [Full Article - PDF]

3845-3851

Crystallographic Analysis of the Binding Modes of Thiazoloisoindolinone Non-Nucleoside Inhibitors to HIV-1 Reverse Transcriptase and Comparison with Modeling Studies Jingshan Ren, Robert M. Esnouf, Andrew L. Hopkins, David I. Stuart, and David K. Stammers [Full Article - PDF]

3852-3859

Novel Inhibitors of Erm Methyltransferases from NMR and Parallel Synthesis Philip J. Hajduk, Jürgen Dinges, Jeffrey M. Schkeryantz, David Janowick, Michele Kaminski, Michael Tufano, David J. Augeri, Andrew Petros, Vicki Nienaber, Ping Zhong, Rachel Hammond, Michael Coen, Bruce Beutel, Leonard Katz, and Stephen W. Fesik [Full Article - PDF]

3860-3873

Substituted Isoquinolines and Quinazolines as Potential Antiinflammatory Agents. Synthesis and Biological Evaluation of Inhibitors of Tumor Necrosis Factor Qi Chao, Lynn Deng, Hsiencheng Shih, Lorenzo M. Leoni, Davide Genini, Dennis A. Carson, and Howard B. Cottam [Full Article - PDF]

3874-3888

Synthesis, Pharmacological and Biophysical Characterization, and Membrane-Interaction QSAR Analysis of Cationic Amphiphilic Model Compounds Christian D. P. Klein, Martin Klingmüller, Christiane Schellinski, Silke Landmann, Stefanie Hauschild, Dieter Heber, Klaus Mohr, and A. J. Hopfinger [Full Article - PDF]

3889-3898

A Combinatorial Approach to the Identification of Dipeptide Aldehyde Inhibitors of -Amyloid Production Jeffrey N. Higaki, Sarvajit Chakravarty, Carmen M. Bryant, Lisa R. Cowart, Paul Harden, Jan Marian Scardina, Babu Mavunkel, Gregory R. Luedtke, and Barbara Cordell [Full Article - PDF]

3899-3909

Glycosylation of Fluoroquinolones through Direct and Oxygenated Polymethylene Linkages as a Sugar-Mediated Active Transport System for Antimicrobials Michael E. Jung, Eric C. Yang, Binh T. Vu, Mehrak Kiankarimi, Emmanouil Spyrou, and Jon Kaunitz [Full Article - PDF]

3910-3918

Conformations of Trypsin-Bound Amidine Inhibitors of Blood Coagulant Factor Xa by Double REDOR NMR and MD Simulations Lynda M. McDowell, Margaret A. McCarrick, Daniel R. Studelska, William J. Guilford, Damian Arnaiz, Jerry L. Dallas, David R. Light, Marc Whitlow, and Jacob Schaefer [Full Article - PDF]

3919-3933

Prospective Identification of Biologically Active Structures by Topomer Shape Similarity Searching Richard D. Cramer, Michael A. Poss, Mark A. Hermsmeier, Thomas J. Caulfield, Mark C. Kowala, and Maria T. Valentine [Full Article - PDF]

3934-3941

Novel 2-Phenylimidazo[1,2-a]pyridine Derivatives as Potent and Selective Ligands for Peripheral Benzodiazepine Receptors: Synthesis, Binding Affinity, and in Vivo Studies Giuseppe Trapani, Massimo Franco, Andrea Latrofa, .Laura Ricciardi, Angelo Carotti, Mariangela Serra, Enrico Sanna, Giovanni Biggio, and Gaetano Liso [Full Article - PDF]

3942-3952

2,4,6-Triarylchalcogenopyrylium Dyes Related in Structure to the Antitumor Agent AA1 as in Vitro Sensitizers for the Photodynamic Therapy of Cancer Kristi A. Leonard, Marina I. Nelen, Linda T. Anderson, Scott L. Gibson, Russell Hilf, and Michael R. Detty [Full Article - PDF]

3953-3964

Synthesis and Evaluation of Chalcogenopyrylium Dyes as Potential Sensitizers for the Photodynamic Therapy of Cancer Kristi A. Leonard, Marina I. Nelen, Todd P. Simard, Sherry R. Davies, Sandra O. Gollnick, Allan R. Oseroff, Scott L. Gibson, Russell Hilf, Lan Bo Chen, and Michael R. Detty [Full Article - PDF]

3965-3970

Synthesis and SAR of 1-Alkyl-2-phenylethylamine Derivatives Designed from N,N-Dipropyl-4-methoxy-3-(2-phenylethoxy)phenylethylamine To Discover 1 Ligands Atsuro Nakazato, Toshihito Kumagai, Kohmei Ohta, Shigeyuki Chaki, Shigeru Okuyama, and Kazuyuki Tomisawa [Full Article - PDF]

3971-3981

Synthesis and Structure-Activity Relationships of Phenylenebis(methylene)- Linked Bis-azamacrocycles That Inhibit HIV-1 and HIV-2 Replication by Antagonism of the Chemokine Receptor CXCR4 Gary J. Bridger, Renato T. Skerlj, Sreenivasan Padmanabhan, Stephen A. Martellucci, Geoffrey W. Henson, Sofie Struyf, Myriam Witvrouw, Dominique Schols, and Erik De Clercq [Full Article - PDF]

3982-3993

Axially Chiral 1,7-Naphthyridine-6-carboxamide Derivatives as Orally Active Tachykinin NK1 Receptor Antagonists: Synthesis, Antagonistic Activity, and Effects on Bladder Functions Hideaki Natsugari, Yoshinori Ikeura, Izumi Kamo, Takenori Ishimaru, Yuji Ishichi, Akira Fujishima, Toshimasa Tanaka, Fumiko Kasahara, Mitsuru Kawada, and Takayuki Doi [Full Article - PDF]

3994-4000

Prodrugs for Amidines: Synthesis and Anti-Pneumocystis carinii Activity of Carbamates of 2,5-Bis(4-amidinophenyl)furan Syed M. Rahmathullah, James Edwin Hall, Brendan C. Bender, Donald R. McCurdy, Richard R. Tidwell, and David W. Boykin [Full Article - PDF]

4001-4009

Combinatorial Library of Serine and Cysteine Protease Inhibitors That Interact with Both the S and S' Binding Sites Paul Abato, Jeffrey L. Conroy, and Christopher T. Seto [Full Article - PDF]

BRIEF ARTICLES

4010-4013

Novel Lipoamino Acid- and Liposaccharide-Based System for Peptide Delivery: Application for Oral Administration of Tumor-Selective Somatostatin Analogues István Tóth, John P. Malkinson, Nicholas S. Flinn, Bruno Drouillat, Anikó Horváth, Judith Érchegyi, Miklós Idei, Anikó Venetianer, Per Artursson, Lucia Lazorova, Béla Szende, and György Kéri [Full Article - PDF]

ADDITIONS AND CORRECTIONS

4014-4014

Non-Peptide GPIIb/IIIa Inhibitors. 20. Centrally Constrained Thienothiophene -Sulfonamides Are Potent, Long Acting in Vivo Inhibitors of Platelet Aggregation Melissa S. Egbertson, Jacquelynn J. Cook, Bohumil Bednar, John D. Prugh, Rodney A. Bednar, Stanley L. Gaul, Robert J. Gould, George D. Hartman, Carl F. Homnick, Marie A. Holahan, Laura A. Libby, Joseph J. Lynch, Jr.,Robert J. Lynch, Gary R. Sitko, Maria T. Stranieri, and Laura M. Vasallo [Full Article - PDF]