EXPEDITED ARTICLES
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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
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ARTICLES
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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 -
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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 -
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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 -
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4313-4324
Free Energy Grids: A Practical Qualitative Application of Free Energy Perturbation to Ligand Design Using the OWFEG Method
David A. Pearlman
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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 -
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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 -
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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 -
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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 -
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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 -
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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 -
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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 -
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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 -
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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]
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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]
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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]
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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]
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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]
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BRIEF ARTICLES
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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]
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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
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BOOK REVIEWS
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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
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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] | |