Journal of Medicinal Chemistry
Volume 41, Issue 9 (April 23, 1998)
Copyright © 1998 American Chemical Society

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COMMUNICATIONS TO THE EDITOR

1357-1360

(-)-6-Chloro-2-[(1-furo[2,3-c]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a New Broad Spectrum HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitor Donn G. Wishka, David R. Graber, Laurice A. Kopta, Robert A. Olmsted, Janice M. Friis, John D. Hosley, Wade J. Adams, Eric P. Seest, Thomas M. Castle, Lester A. Dolak, Barbara J. Keiser, Yoshihiko Yagi, Azhwarsamy Jeganathan, Stephen T. Schlachter, Michael J. Murphy, Gary J. Cleek, Richard A. Nugent, Susan M. Poppe, Steven M. Swaney, Fusen Han, William Watt, Wendy L. White, Toni-Jo Poel, Richard C. Thomas, Richard L. Voorman, Kevin J. Stefanski, Randall G. Stehle, W. Gary Tarpley, and Joel Morris [Full Article - PDF]

EXPEDITED ARTICLES

1361-1366

2-Iminohomopiperidinium Salts as Selective Inhibitors of Inducible Nitric Oxide Synthase (iNOS) Donald W. Hansen, Jr., Karen B. Peterson, Mahima Trivedi, Steven W. Kramer, Ronald K. Webber, Foe S. Tjoeng, William M. Moore, Gina M. Jerome, Christine M. Kornmeier, Pamela T. Manning, Jane R. Connor, Thomas P. Misko, Mark G. Currie, and Barnett S. Pitzele [Full Article - PDF]

1367-1370

Rational Drug Design Approach for Overcoming Drug Resistance: Application to Pyrimethamine Resistance in Malaria James H. McKie, Kenneth T. Douglas, Cecil Chan, Simon A. Roser, Robert Yates, Martin Read, John E. Hyde, Michael J. Dascombe, Yongyuth Yuthavong, and Worachart Sirawaraporn [Full Article - PDF]

1371-1381

Anti-HIV Agents That Selectively Target Retroviral Nucleocapsid Protein Zinc Fingers without Affecting Cellular Zinc Finger Proteins Mingjun Huang, Andrew Maynard, Jim A. Turpin, Lisa Graham, George M. Janini, David G. Covell, and William G. Rice [Full Article - PDF]

1382-1391

Modulation of Receptor and Receptor Subtype Affinities Using Diastereomeric and Enantiomeric Monosaccharide Scaffolds as a Means to Structural and Biological Diversity. A New Route to Ether Synthesis Ralph Hirschmann, John Hynes, Jr., Maria A. Cichy-Knight, Rachel D. van Rijn, Paul A. Sprengeler, P. Grant Spoors, William C. Shakespeare, Sherrie Pietranico-Cole, Joseph Barbosa, Josephine Liu, Wenqing Yao, Susan Rohrer, and Amos B. Smith, III [Full Article - PDF]

ARTICLES

1392-1398

Effect of Steroids on DNA Synthesis in an in Vitro Replication System: Initial Quantitative Structure-Activity Relationship Studies and Construction of a Non-Estrogen Receptor Pharmacophore Kamal Azzaoui, Maria J. Diaz-Perez, Maria Zannis-Hadjoupoulos, Gerry B. Price, and Irving W. Wainer [Full Article - PDF]

1399-1408

Novel Tetranuclear Orthometalated Complexes of Pd(II) and Pt(II) Derived from p-Isopropylbenzaldehyde Thiosemicarbazone with Cytotoxic Activity in cis-DDP Resistant Tumor Cell Lines. Interaction of These Complexes with DNA Adoración G. Quiroga, José M. Pérez, Isabel López-Solera, José R. Masaguer, Antonio Luque, Pascual Román, Andy Edwards, Carlos Alonso, and Carmen Navarro-Ranninger [Full Article - PDF]

1409-1416

Synthesis and Biological Activities of Tricyclic Conformationally Restricted Tetrahydropyrido Annulated Furo[2,3-d]pyrimidines as Inhibitors of Dihydrofolate Reductases Aleem Gangjee, Elfatih Elzein, Sherry F. Queener, and John J. McGuire [Full Article - PDF]

1417-1427

cycloSal-2',3'-dideoxy-2',3'-didehydrothymidine Monophosphate (cycloSal-d4TMP): Synthesis and Antiviral Evaluation of a New d4TMP Delivery System Chris Meier, Martina Lorey, Erik De Clercq, and Jan Balzarini [Full Article - PDF]

1428-1438

Synthesis and Structure-Activity Relationships of Carboxyflavones as Structurally Rigid CysLT1 (LTD4) Receptor Antagonists Mariël E. Zwaagstra, Henk Timmerman, Andrea C. van de Stolpe, Frans J. J. de Kanter, Masahiro Tamura, Yasushi Wada, and Ming-Qiang Zhang [Full Article - PDF]

1439-1445

Development of a Three-Dimensional CysLT1 (LTD4) Antagonist Model with an Incorporated Amino Acid Residue from the Receptor Mariël E. Zwaagstra, Saskia H. H. F. Schoenmakers, Paul H. J. Nederkoorn, Edith Gelens, Henk Timmerman, and Ming-Qiang Zhang [Full Article - PDF]

1446-1455

Nonpeptide Cyclic Cyanoguanidines as HIV-1 Protease Inhibitors: Synthesis, Structure-Activity Relationships, and X-ray Crystal Structure Studies Prabhakar K. Jadhav, Francis J. Woerner, Patrick Y. S. Lam, C. Nicholas Hodge, Charles J. Eyermann, Hon-Wah Man, Wayne F. Daneker, Lee T. Bacheler, Marlene M. Rayner, James L. Meek, Susan Erickson-Viitanen, David A. Jackson, Joseph C. Calabrese, Margaret Schadt, and Chong-Hwan Chang [Full Article - PDF]

1456-1466

Human P2Y1 Receptor: Molecular Modeling and Site-Directed Mutagenesis as Tools To Identify Agonist and Antagonist Recognition Sites Stefano Moro, Danping Guo, Emidio Camaioni, José L. Boyer, T. Kendall Harden, and Kenneth A. Jacobson [Full Article - PDF]

1467-1475

Conformation-Function Relationship of Vitamin D: Conformational Analysis Predicts Potential Side-Chain Structure Sachiko Yamada, Keiko Yamamoto, Hiroyuki Masuno, and Masateru Ohta [Full Article - PDF]

1476-1496

Clarification of the Binding Mode of Teleocidin and Benzolactams to the Cys2 Domain of Protein Kinase C by Synthesis of Hydrophobically Modified, Teleocidin-Mimicking Benzolactams and Computational Docking Simulation Yasuyuki Endo, Shunji Takehana, Michihiro Ohno, Paul E. Driedger, Silvia Stabel, Miho Y. Mizutani, Nobuo Tomioka, Akiko Itai, and Koichi Shudo [Full Article - PDF]

1497-1506

Membrane-Induced Secondary Structures of Neuropeptides: A Comparison of the Solution Conformations Adopted by Agonists and Antagonists of the Mammalian Tachykinin NK1 Receptor Tracy L. Whitehead, Sharon D. McNair, Chad E. Hadden, John K. Young, and Rickey P. Hicks [Full Article - PDF]

1507-1512

Therapeutic Effects of Monoclonal Antibody--Lactamase Conjugates in Combination with a Nitrogen Mustard Anticancer Prodrug in Models of Human Renal Cell Carcinoma Håkan P. Svensson, Ian S. Frank, Karen K. Berry, and Peter D. Senter [Full Article - PDF]

1513-1523

Design and Synthesis of Potent, Selective Inhibitors of Endothelin-Converting Enzyme Eli M. Wallace, John A. Moliterni, Michael A. Moskal, Alan D. Neubert, Nicholas Marcopulos, Lisa B. Stamford, Angelo J. Trapani, Paula Savage, Mary Chou, and Arco Y. Jeng [Full Article - PDF]

1524-1530

Synthesis and Biological Activity of Chimeric Structures Derived from the Cytotoxic Natural Compounds Dolastatin 10 and Dolastatin 15 Joël Poncet, Magali Busquet, Florence Roux, Alain Pierré, Ghanem Atassi, and Patrick Jouin [Full Article - PDF]

1531-1539

Nuclease-Resistant Composite 2',5'-Oligoadenylate-3',5'-Oligonucleotides for the Targeted Destruction of RNA: 2-5A-Iso-antisense Wei Xiao, Guiying Li, Mark R. Player, Ratan K. Maitra, Cornelius F. Waller, Robert H. Silverman, and Paul F. Torrence [Full Article - PDF]

1540-1554

Structure-Activity Relationship of New Growth Inhibitors of Trypanosoma cruzi Güendalina M. Cinque, Sergio H. Szajnman, Li Zhong, Roberto Docampo, Andrea J. Schvartzapel, Juan B. Rodriguez, and Eduardo G. Gros [Full Article - PDF]

BOOK REVIEWS

1555-1556

Reviews in Computational Chemistry, Volume 10 Edited by Kenny B. Lipkowitz and Donald B. Boyd. VCH Publishers, Inc., New York. 1997. xxiii + 334 pp. 16 × 24 cm. ISBN 1-56081-957-X. $120.00. M. Katharine Holloway [Full Article - PDF]

1556-1556

The Impact of Stereochemistry on Drug Development and Use. Volume 142 in Chemical Analysis. Edited by H. Y. Aboul-Enein and I. W. Wainer. John Wiley & Sons, New York. 1997. xxvii + 695 pp. 16 × 23.5 cm. ISBN 0-471-59644-2. $99.00 David E. Nichols [Full Article - PDF]