ANNOUNCEMENT
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4015-4015
2000-2001 Predoctoral Fellowships
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EXPEDITED ARTICLES
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4016-4020
Diethylcarbamoylating/Nitroxylating Agents as Dual Action Inhibitors of Aldehyde Dehydrogenase: A Disulfiram-Cyanamide Merger
Terry T. Conway,
Eugene G. DeMaster,
David J. W. Goon,
Frances N. Shirota, and
Herbert T. Nagasawa
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ARTICLES
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4021-4027
High-Resolution NMR and Computer Modeling Studies of the Cannabimimetic Aminoalkylindole Prototype WIN-55212-2
Xiang-Qun Xie,
Xiu-Wen Han,
Jian-Zhong Chen,
Michael Eissenstat, and
Alexandros Makriyannis
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4028-4041
Design, Synthesis, and Evaluation of a Novel Sequence-Selective Epoxide-Containing DNA Cross-Linking Agent Based on the Pyrrolo[2,1-c][1,4]benzodiazepine System
Stuart C. Wilson,
Philip W. Howard,
Stephen M. Forrow,
John A. Hartley,
Lesley J. Adams,
Terence C. Jenkins,
Lloyd R. Kelland, and
David E. Thurston
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4042-4053
Synthesis and Antiviral Activity of Ethidium-Arginine Conjugates Directed Against the TAR RNA of HIV-1
Valérie Peytou,
Roger Condom,
Nadia Patino,
Roger Guedj,
Anne-Marie Aubertin,
Nathalie Gelus,
Christian Bailly,
Raphaël Terreux, and
Daniel Cabrol-Bass
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4054-4061
Inhibitors of the C2-Symmetric HIV-1 Protease: Nonsymmetric Binding of a Symmetric Cyclic Sulfamide with Ketoxime Groups in the P2/P2' Side Chains
Johan Hultén,
Hans O. Andersson,
Wesley Schaal,
Helena U. Danielson,
Björn Classon,
Ingemar Kvarnström,
Anders Karlén,
Torsten Unge,
Bertil Samuelsson, and
Anders Hallberg
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4062-4070
A Novel Approach to Predicting P450 Mediated Drug Metabolism. CYP2D6 Catalyzed N-Dealkylation Reactions and Qualitative Metabolite Predictions Using a Combined Protein and Pharmacophore Model for CYP2D6
Marcel J. de Groot,
Mark J. Ackland,
Valerie A. Horne,
Alexander A. Alex, and
Barry C. Jones
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4071-4080
Bioreductive Activation of a Series of Indolequinones by Human DT-Diaphorase: Structure-Activity Relationships
Roger M. Phillips,
Matthew A. Naylor,
Mohammed Jaffar,
Stephen W. Doughty,
Steven A. Everett,
Anthony G. Breen,
Guzanfar A. Choudry, and
Ian J. Stratford
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4081-4087
Antitumor Agents. 196. Substituted 2-Thienyl-1,8-naphthyridin-4-ones: Their Synthesis, Cytotoxicity, and Inhibition of Tubulin Polymerization
Shun-Xiang Zhang,
Kenneth F. Bastow,
Yoko Tachibana,
Sheng-Chu Kuo,
Ernest Hamel,
Anthony Mauger,
Ven L. Narayanan, and
Kuo-Hsiung Lee
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4088-4098
Discovery of Potent and Selective SH2 Inhibitors of the Tyrosine Kinase ZAP-70
Chi B. Vu,
Evelyn G. Corpuz,
Taylor J. Merry,
Selvaluxmi G. Pradeepan,
Catherine Bartlett,
Regine S. Bohacek,
Martyn C. Botfield,
Charles J. Eyermann,
Berkley A. Lynch,
Ian A. MacNeil,
Mary K. Ram,
Marie Rose van Schravendijk,
Shelia Violette, and
Tomi K. Sawyer
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4099-4107
Synthesis and Enantiopharmacology of New AMPA-Kainate Receptor Agonists
Paola Conti,
Marco De Amici,
Giovambattista De Sarro,
Milena Rizzo,
Tine Bryan Stensbl,
Hans Bräuner-Osborne,
Ulf Madsen,
Lucio Toma, and
Carlo De Micheli
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4108-4121
Inhibition of Neuronal Nitric Oxide Synthase by 4-Amino Pteridine Derivatives: Structure-Activity Relationship of Antagonists of (6R)-5,6,7,8-Tetrahydrobiopterin Cofactor
Lothar G. Fröhlich,
Peter Kotsonis,
Hermann Traub,
Shahriyar Taghavi-Moghadam,
Najim Al-Masoudi,
Heinrich Hofmann,
Hartmut Strobel,
Hans Matter,
Wolfgang Pfleiderer, and
Harald H. H. W. Schmidt
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4122-4128
Design and Synthesis of Lipophilic Phosphoramidate d4T-MP Prodrugs Expressing High Potency Against HIV in Cell Culture: Structural Determinants for in Vitro Activity and QSAR
Adam Q. Siddiqui,
Christopher McGuigan,
Carlo Ballatore,
Fabio Zuccotto,
Ian H. Gilbert,
Erik De Clercq, and
Jan Balzarini
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4129-4139
Protein Kinase C Ligands Based on Tetrahydrofuran Templates Containing a New Set of Phorbol Ester Pharmacophores
Jeewoo Lee,
Ji-Hye Kang,
Sang-Yoon Lee,
Kee-Chung Han,
Christina M. Torres,
Dipak K. Bhattacharyya,
Peter M. Blumberg, and
Victor E. Marquez
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4140-4149
Synthesis and Structure-Activity Relationships of the (Alkylamino)piperidine-Containing BHAP Class of Non-Nucleoside Reverse Transcriptase Inhibitors: Effect of 3-Alkylpyridine Ring Substitution
Michael J. Genin,
Toni J. Poel,
Paul D. May,
Laurice A. Kopta,
Yoshihiko Yagi,
Robert A. Olmsted,
Janice M. Friis,
Richard L. Voorman,
Wade J. Adams,
Richard C. Thomas, and
Donna L. Romero
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4150-4160
Urea-PETT Compounds as a New Class of HIV-1 Reverse Transcriptase Inhibitors. 3. Synthesis and Further Structure-Activity Relationship Studies of PETT Analogues
Marita Högberg,
Christer Sahlberg,
Per Engelhardt,
Rolf Noréen,
Jussi Kangasmetsä,
Nils Gunnar Johansson,
Bo Öberg,
Lotta Vrang,
Hong Zhang,
Britt-Louise Sahlberg,
Torsten Unge,
Seved Lövgren,
Kerstin Fridborg, and
Kristina Bäckbro
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4161-4171
6-Substituted 2-Oxo-2H-1-benzopyran-3-carboxylic Acid as a Core Structure for Specific Inhibitors of Human Leukocyte Elastase
Caroline Doucet,
Lionel Pochet,
Nicole Thierry,
Bernard Pirotte,
Jacques Delarge, and
Michèle Reboud-Ravaux
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4172-4184
Antitumor Benzothiazoles. 8. Synthesis, Metabolic Formation, and Biological Properties of the C- and N-Oxidation Products of Antitumor 2-(4-Aminophenyl)benzothiazoles
Eiji Kashiyama,
Ian Hutchinson,
Mei-Sze Chua,
Sherman F. Stinson,
Lawrence R. Phillips,
Gurmeet Kaur,
Edward A. Sausville,
Tracey D. Bradshaw,
Andrew D. Westwell, and
Malcolm F. G. Stevens
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4185-4192
Design and Synthesis of Potent Bradykinin Agonists Containing a Benzothiazepine Moiety
Muriel Amblard,
Isabelle Daffix,
Philippe Bedos,
Gilbert Bergé,
Didier Pruneau,
Jean-Luc Paquet,
Jean-Michel Luccarini,
Pierre Bélichard,
Pierre Dodey, and
Jean Martinez
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4193-4201
Synthesis and Characterization of Bradykinin B2 Receptor Agonists Containing Constrained Dipeptide Mimics
Muriel Amblard,
Isabelle Daffix,
Gilbert Bergé,
Monique Calmès,
Pierre Dodey,
Didier Pruneau,
Jean-Luc Paquet,
Jean-Michel Luccarini,
Pierre Bélichard, and
Jean Martinez
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4202-4213
Synthesis and Antimicrobial Activity of 4H-4-Oxoquinolizine Derivatives: Consequences of Structural Modification at the C-8 Position
Zhenkun Ma,
Daniel T. W. Chu,
Curt S. Cooper,
Qun Li,
Anthony K. L. Fung,
Sanyi Wang,
Linus L. Shen,
Robert K. Flamm,
Angela M. Nilius,
Jeffery D. Alder,
Jonathan A. Meulbroek, and
Yat Sun Or
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4214-4224
WB 4101-Related Compounds. 2. Role of the Ethylene Chain Separating Amine and Phenoxy Units on the Affinity for 1-Adrenoreceptor Subtypes and 5-HT1A Receptors
Maria L. Bolognesi,
Roberta Budriesi,
Andrea Cavalli,
Alberto Chiarini,
Roberto Gotti,
Amedeo Leonardi,
Anna Minarini,
Elena Poggesi,
Maurizio Recanatini,
Michela Rosini,
Vincenzo Tumiatti, and
Carlo Melchiorre
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4225-4231
Heterodimeric Tacrine-Based Acetylcholinesterase Inhibitors: Investigating Ligand-Peripheral Site Interactions
Paul R. Carlier,
Ella S.-H. Chow,
Yifan Han,
Jing Liu,
Jamal El Yazal, and
Yuan-Ping Pang
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4232-4238
Selective A3 Adenosine Receptor Antagonists: Water-Soluble 3,5-Diacyl-1,2,4-trialkylpyridinium Salts and Their Oxidative Generation from Dihydropyridine Precursors
Rongyuan Xie,
An-Hu Li,
Xiao-Duo Ji,
Neli Melman,
Mark E. Olah,
Gary L. Stiles, and
Kenneth A. Jacobson
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4239-4249
Synthesis of a Series of 4-Benzyloxyaniline Analogues as Neuronal N-Type Calcium Channel Blockers with Improved Anticonvulsant and Analgesic Properties
Lain-Yen Hu,
Todd R. Ryder,
Michael F. Rafferty,
M. Rose Feng,
Susan M. Lotarski,
David M. Rock,
Michael Sinz,
Sally J. Stoehr,
Charles P. Taylor,
Mark L. Weber,
S. Scott Bowersox,
George P. Miljanich,
Elizabeth Millerman,
Yong-Xiang Wang, and
Balazs G. Szoke
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4250-4256
3-Alkyl-6-Chloro-2-pyrones: Selective Inhibitors of Pancreatic Cholesterol Esterase
Lorraine M. Deck,
Miranda L. Baca,
Stephanie L. Salas,
Lucy A. Hunsaker, and
David L. Vander Jagt
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4257-4263
Further Studies on Oxygenated Tryptamines with LSD-like Activity Incorporating a Chiral Pyrrolidine Moiety into the Side Chain
Madina Gerasimov,
Danuta Marona-Lewicka,
Deborah M. Kurrasch-Orbaugh,
Amjad M. Qandil, and
David E. Nichols
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BRIEF ARTICLES
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4264-4268
Preparation and Characterization of Novel trans-[PtCl2(amine)(isopropylamine)] Compounds: Cytotoxic Activity and Apoptosis Induction in ras-Transformed Cells
Eva I. Montero,
Sonia Díaz,
Ana Ma González-Vadillo,
José M. Pérez,
C. Alonso, and
Carmen Navarro-Ranninger
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4269-4274
Novel Partial Agonists for the Histamine H3 Receptor with High in Vitro and in Vivo Activity
Astrid Sasse,
Holger Stark,
Sibylle Reidemeister,
Annette Hüls,
Sigurd Elz,
Xavier Ligneau,
C. Robin Ganellin,
Jean-Charles Schwartz, and
Walter Schunack
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