Journal of Medicinal Chemistry
Volume 42, Issue 21 (October 21, 1999)
Copyright © 1999 American Chemical Society

Click [Full Article - PDF] to display or print the full article page image in PDF.

EXPEDITED ARTICLES

4275-4280

Antimalarial, Antiproliferative, and Antitumor Activities of Artemisinin-Derived, Chemically Robust, Trioxane Dimers Gary H. Posner, Poonsakdi Ploypradith, Michael H. Parker,,1a Hardwin O'Dowd, Soon-Hyung Woo,,1b John Northrop,,1c Mikhail Krasavin, Patrick Dolan, Thomas W. Kensler, Suji Xie, and Theresa A. Shapiro [Full Article - PDF]

ARTICLES

4281-4291

Synthesis of Novel GABA Uptake Inhibitors. 4. Bioisosteric Transformation and Successive Optimization of Known GABA Uptake Inhibitors Leading to a Series of Potent Anticonvulsant Drug Candidates Knud Erik Andersen, Jan L. Srensen, Per O. Huusfeldt, Lars J. S. Knutsen, Jesper Lau, Behrend F. Lundt, Hans Petersen, Peter D. Suzdak, and Michael D. B. Swedberg [Full Article - PDF]

4292-4299

Novel Series of Non-Glycerol-Based Cationic Transfection Lipids for Use in Liposomal Gene Delivery Rajkumar Banerjee, Prasanta Kumar Das, Gollapudi Venkata Srilakshmi, and Arabinda Chaudhuri , Nalam Madhusudhana Rao [Full Article - PDF]

4300-4312

Design, Synthesis, and Evaluation of Inhibitors of Trypanosomal and Leishmanial Dihydrofolate Reductase Shafinaz F. Chowdhury, Victor Bernier Villamor, Ramon Hurtado Guerrero, Isabel Leal, Reto Brun, Simon L. Croft, Jonathan M. Goodman, Louis Maes, Luis M. Ruiz-Perez, Dolores Gonzalez Pacanowska, and Ian H. Gilbert [Full Article - PDF]

4313-4324

Free Energy Grids: A Practical Qualitative Application of Free Energy Perturbation to Ligand Design Using the OWFEG Method David A. Pearlman [Full Article - PDF]

4325-4330

Crystal Structure of Human DT-diaphorase: A Model for Interaction with the Cytotoxic Prodrug 5-(Aziridin-1-yl)-2,4-dinitrobenzamide (CB1954) Jane V. Skelly, Mark R. Sanderson, David A. Suter, Ulrich Baumann, Martin A. Read, David S. J. Gregory, Matthew Bennett, Stephen M. Hobbs, and Stephen Neidle [Full Article - PDF]

4331-4342

Design, Synthesis, and Evaluation of Phe-Gly Mimetics: Heterocyclic Building Blocks for Pseudopeptides Susanna Borg, Roeland C. Vollinga, Maryse Labarre, Kemal Payza, Lars Terenius, and Kristina Luthman [Full Article - PDF]

4343-4350

Structure-Activity Relationships and Molecular Modeling Analysis of Flavonoids Binding to the Benzodiazepine Site of the Rat Brain GABAA Receptor Complex Kim Dekermendjian, Pia Kahnberg, Michael-Robin Witt, Olov Sterner, Mogens Nielsen, and Tommy Liljefors [Full Article - PDF]

4351-4361

Enantiospecific Synthesis of 3-Fluoromethyl-, 3-Hydroxymethyl-, and 3-Chloromethyl-1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the 2-Adrenoceptor Gary L. Grunewald, Timothy M. Caldwell, Qifang Li, Vilas H. Dahanukar, Brynn McNeil, and Kevin R. Criscione [Full Article - PDF]

4362-4379

Pyrroloquinoxaline Derivatives as High-Affinity and Selective 5-HT3 Receptor Agonists: Synthesis, Further Structure-Activity Relationships, and Biological Studies Giuseppe Campiani, Elena Morelli, Sandra Gemma, Vito Nacci, Stefania Butini, Michel Hamon, Ettore Novellino, Giovanni Greco, Alfredo Cagnotto, Mara Goegan, Luigi Cervo, Fabio Dalla Valle, Claudia Fracasso, Silvio Caccia, and Tiziana Mennini [Full Article - PDF]

4380-4387

Compounds That Activate the Mouse Melanocortin-1 Receptor Identified by Screening a Small Molecule Library Based upon the -Turn Carrie Haskell-Luevano, Åsa Rosenquist, Andrew Souers, Kathy C. Khong, Jonathon A. Ellman, and Roger D. Cone [Full Article - PDF]

4388-4393

New Natural Sesquiterpenes as Modulators of Daunomycin Resistance in a Multidrug-Resistant Leishmania tropica Line José M. Pérez-Victoria, Benigna M. Tincusi, Ignacio A. Jiménez, Isabel L. Bazzocchi, Mahabir P. Gupta, Santiago Castanys, Francisco Gamarro, and Angel G. Ravelo [Full Article - PDF]

4394-4404

Evaluation and Biological Properties of Reactive Ligands for the Mapping of the Glycine Site on the N-Methyl-D-aspartate (NMDA) Receptor Annett Kreimeyer, Bodo Laube, Mike Sturgess, Maurice Goeldner, and Bernard Foucaud [Full Article - PDF]

4405-4413

New Tetracyclic Analogues of Photochemotherapeutic Drugs 5-MOP and 8-MOP: Synthesis, DNA Interaction, and Antiproliferative Activity Lisa Dalla Via, Ornella Gia, Sebastiano Marciani Magno, Lourdes Santana, Marta Teijeira, and Eugenio Uriarte [Full Article - PDF]

4414-4421

Synthesis and Anticonvulsant Activity of Novel and Potent 2,3-Benzodiazepine AMPA/Kainate Receptor Antagonists Silvana Grasso, Giovambattista De Sarro, Angela De Sarro, Nicola Micale, Maria Zappalà, Giulia Puia, Mario Baraldi, and Carlo De Micheli [Full Article - PDF]

4422-4433

Two-Stage Method for Protein-Ligand Docking Daniel Hoffmann, Bernd Kramer, Takumi Washio, Torsten Steinmetzer, Matthias Rarey, and Thomas Lengauer [Full Article - PDF]

4434-4445

Heteroarotinoids Inhibit Head and Neck Cancer Cell Lines in Vitro and in Vivo Through Both RAR and RXR Retinoic Acid Receptors David Zacheis, Arindam Dhar, Shennan Lu, Matora M. Madler, Jozef Klucik, Chad W. Brown, Shengquan Liu, Francis Clement, Shankar Subramanian, G. Mahika Weerasekare, K. Darrell Berlin, Michael A. Gold, John R. Houck, Jr., Kenneth R. Fountain, and Doris M. Benbrook [Full Article - PDF]

4446-4455

Structure-Activity Relationships at the Monoamine Transporters and Receptors for a Novel Series of 9-[3-(cis-3,5-Dimethyl-1-piperazinyl)-propyl]carbazole (Rimcazole) Analogues Stephen M. Husbands, Sari Izenwasser, Theresa Kopajtic, Wayne D. Bowen, Bertold J. Vilner, Jonathan L. Katz, and Amy Hauck Newman [Full Article - PDF]

BRIEF ARTICLES

4456-4461

Retention of Immunosuppressant Activity in an Ascomycin Analogue Lacking a Hydrogen-Bonding Interaction with FKBP12 Paul E. Wiedeman, Stephen W. Fesik, Andrew M. Petros, David G. Nettesheim, Karl W. Mollison, Benjamin C. Lane, Yat Sun Or, and Jay R. Luly [Full Article - PDF]

4462-4470

Pyrrolobenzoxazepinone Derivatives as Non-Nucleoside HIV-1 RT Inhibitors: Further Structure-Activity Relationship Studies and Identification of More Potent Broad-Spectrum HIV-1 RT Inhibitors with Antiviral Activity Giuseppe Campiani, Elena Morelli, Monica Fabbrini, Vito Nacci, Giovanni Greco, Ettore Novellino, Anna Ramunno, Giovanni Maga, Silvio Spadari, Giuseppe Caliendo, Alberto Bergamini, Emanuela Faggioli, Ilaria Uccella, Francesca Bolacchi, Stefano Marini, Massimiliano Coletta, Angelo Nacca, and Silvio Caccia [Full Article - PDF]

BOOK REVIEWS

4471-4471

Handbook of Drug Metabolism Edited by Thomas F. Woolf. Marcel Dekker, New York. 1999. xi + 596 pp. 18 × 26 cm. ISBN 0-8247-0229-8. $225.00. Michael W. Duffel [Full Article - PDF]

4472-4472

Protein Purification. Principles, High-Resolution Methods, and Applications. 2nd Edition Edited by Jan-Christer Janson and Lars Ryden. Wiley-Liss, John Wiley & Sons, Inc., New York. 1998. x + 695 pp. 16 x 24 cm. ISBN 0-471-18626-0. $74.95. A. H. Nishikawa [Full Article - PDF]