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COMMUNICATIONS
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2971-2974
Identification of a Chemical Tool for the Orphan Nuclear Receptor FXR
Patrick R. Maloney,
Derek J. Parks,
Curt D. Haffner,
Adam M. Fivush,
Gyan Chandra,
Kelli D. Plunket,
Katrina L. Creech,
Linda B. Moore,
Joan G. Wilson,
Michael C. Lewis,
Stacey A. Jones, and
Timothy M. Willson
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EXPEDITED ARTICLES
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2975-2981
3,5-Bis(trifluoromethyl)pyrazoles: A Novel Class of NFAT Transcription Factor Regulator
Stevan W. Djuric,
Nwe Y. BaMaung,
Anwer Basha,
Huaqing Liu,
Jay R. Luly,
David J. Madar,
Richard J. Sciotti,
Noah P. Tu,
Frank L. Wagenaar,
Paul E. Wiedeman,
Xun Zhou,
Stephen Ballaron,
Joy Bauch,
Yung-Wu Chen,
X. Grace Chiou,
Thomas Fey,
Donna Gauvin,
Earl Gubbins,
Gin C. Hsieh,
Kennan C. Marsh,
Karl W. Mollison,
Melissa Pong,
Thomas K. Shaughnessy,
Michael P. Sheets,
Morey Smith,
James M. Trevillyan,
Usha Warrior,
Craig D. Wegner, and
George W. Carter[Full Article -
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2982-2991
2-Carbomethoxy-3-aryl-8-bicyclo[3.2.1]octanes: Potent Non-Nitrogen Inhibitors of Monoamine Transporters
Peter C. Meltzer,
Paul Blundell,
Yaw F. Yong,
Zhengming Chen,
Clifford George,
Mario D. Gonzalez, and
Bertha K. Madras[Full Article -
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ARTICLES
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2992-3004
Nonpeptide Analogues of Dynorphin A(1-8): Design, Synthesis, and Pharmacological Evaluation of  -Selective Agonists
Giuseppe Ronsisvalle,
Lorella Pasquinucci,
Valeria Pittalà,
Agostino Marrazzo,
Orazio Prezzavento,
Rosanna Di Toro,
Barbara Falcucci, and
Santi Spampinato[Full Article -
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3005-3019
CoMFA-Based Prediction of Agonist Affinities at Recombinant Wild Type versus Serine to Alanine Point Mutated D2 Dopamine Receptors
Richard E. Wilcox,
Wen-Hsin Huang,
Mi-Youn Kim Brusniak,
David M. Wilcox,
Robert S. Pearlman,
Martha M. Teeter,
Curtiss J. DuRand,
Brenda L. Wiens, and
Kim A. Neve[Full Article -
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3020-3032
DoMCoSAR: A Novel Approach for Establishing the Docking Mode That Is Consistent with the Structure-Activity Relationship. Application to HIV-1 Protease Inhibitors and VEGF Receptor Tyrosine Kinase Inhibitors
Michal Vieth and
David J. Cummins[Full Article -
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3033-3044
GRID/CPCA: A New Computational Tool To Design Selective Ligands
Mika A. Kastenholz,
Manuel Pastor,
Gabriele Cruciani,
Eric E. J. Haaksma, and
Thomas Fox[Full Article -
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3045-3051
3-(Hydroxymethyl)-Bearing Phosphatidylinositol Ether Lipid Analogues and Carbonate Surrogates Block PI3-K, Akt, and Cancer Cell Growth
Youhong Hu,
Lixin Qiao,
Shaomeng Wang,
Suo-bao Rong,
Emmanuelle J. Meuillet,
Margareta Berggren,
Alfred Gallegos,
Garth Powis, and
Alan P. Kozikowski[Full Article -
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3052-3066
Molecular Design, Synthesis, and Hypoglycemic Activity of a Series of Thiazolidine-2,4-diones
Minoru Oguchi,
Kunio Wada,
Hidehito Honma,
Asako Tanaka,
Tomoko Kaneko,
Sachiko Sakakibara,
Jun Ohsumi,
Nobufusa Serizawa,
Toshihiko Fujiwara,
Hiroyoshi Horikoshi, and
Takashi Fujita[Full Article -
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3067-3073
Analogues of Amonafide and Azonafide with Novel Ring Systems
Salah M. Sami,
Robert T. Dorr,
David S. Alberts,
Anikó M. Sólyom, and
William A. Remers[Full Article -
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3074-3084
1-[4-(3-Phenylalkyl)phenyl]-2-aminopropanes as 5-HT2A Partial Agonists
Cynthia S. Dowd,
Katharine Herrick-Davis,
Christina Egan,
Ann DuPre,
Carol Smith,
Milt Teitler, and
Richard A. Glennon[Full Article -
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3085-3092
Structure-Function Studies of Polymyxin B Nonapeptide: Implications to Sensitization of Gram-Negative Bacteria
Haim Tsubery,
Itzhak Ofek,
Sofia Cohen, and
Mati Fridkin[Full Article -
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3093-3102
Synthesis and Biological Evaluation of 2'-Carbamate-Linked and 2'-Carbonate-Linked Prodrugs of Paclitaxel: Selective Activation by the Tumor-Associated Protease Plasmin
Franciscus M. H. de Groot,
Leon W. A. van Berkom, and
Hans W. Scheeren[Full Article -
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3103-3110
Novel Radiotracers for Imaging the Serotonin Transporter by Positron Emission Tomography: Synthesis, Radiosynthesis, and in Vitro and ex Vivo Evaluation of 11C-Labeled 2-(Phenylthio)araalkylamines
Alan A. Wilson,
Nathalie Ginovart,
Mark Schmidt,
Jeffery H. Meyer,
Penny G. Threlkeld, and
Sylvain Houle[Full Article -
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3111-3117
Biphenylsulfonamide Endothelin Receptor Antagonists. 2. Discovery of 4'-Oxazolyl Biphenylsulfonamides as a New Class of Potent, Highly Selective ETA Antagonists
Natesan Murugesan,
Zhengxiang Gu,
Philip D. Stein,
Steven Spergel,
Arvind Mathur,
Leslie Leith,
Eddie C.-K. Liu,
Rongan Zhang,
Eileen Bird,
Tom Waldron,
Anthony Marino,
Richard A. Morrison,
Maria L. Webb,
Suzanne Moreland, and
Joel C. Barrish[Full Article -
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3118-3124
Synthesis and Structure-Activity Relationships of a New Set of 2-Arylpyrazolo[3,4-c]quinoline Derivatives as Adenosine Receptor Antagonists
Vittoria Colotta,
Daniela Catarzi,
Flavia Varano,
Lucia Cecchi,
Guido Filacchioni,
Claudia Martini,
Letizia Trincavelli, and
Antonio Lucacchini[Full Article -
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3125-3133
Effect of C9-Methyl Substitution and C8-C9 Conformational Restriction on Antifolate and Antitumor Activity of Classical 5-Substituted 2,4-Diaminofuro[2,3-d]pyrimidines
Aleem Gangjee,
Yibin Zeng,
John J. McGuire, and
Roy L. Kisliuk[Full Article -
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3134-3147
Synthesis and Structure-Activity Relationships of 7-Substituted 3-(2,6-Dichlorophenyl)-1,6-naphthyridin-2(1H)-ones as Selective Inhibitors of pp60c-src
Andrew M. Thompson,
Gordon W. Rewcastle,
Stacey L. Boushelle,
Brian G. Hartl,
Alan J. Kraker,
Gina H. Lu,
Brian L. Batley,
Robert L. Panek,
H. D. Hollis Showalter, and
William A. Denny[Full Article -
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3148-3156
Use of an Additional Hydrophobic Binding Site, the Z Site, in the Rational Drug Design of a New Class of Stronger Trypanothione Reductase Inhibitor, Quaternary Alkylammonium Phenothiazines
M. Omar F. Khan,
Susan E. Austin,
Cecil Chan,
Hong Yin,
Debora Marks,
Sheetal N. Vaghjiani,
Howard Kendrick,
Vanessa Yardley,
Simon L. Croft, and
Kenneth T. Douglas[Full Article -
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3157-3167
Development of Novel Quinone Phosphorodiamidate Prodrugs Targeted to DT-Diaphorase
Carolee Flader,
Jiwen Liu, and
Richard F. Borch[Full Article -
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3168-3185
Selective Cyclooxygenase-2 Inhibitors: Heteroaryl Modified 1,2-Diarylimidazoles Are Potent, Orally Active Antiinflammatory Agents
Ish K. Khanna,
Yi Yu,
Renee M. Huff,
Richard M. Weier,
Xiangdong Xu,
Francis J. Koszyk,
Paul W. Collins,
J. Nita Cogburn,
Peter C. Isakson,
Carol M. Koboldt,
Jaime L. Masferrer,
William E. Perkins,
Karen Seibert,
Amy W. Veenhuizen,
Jinhua Yuan,
Dai-Chang Yang, and
Yan Y. Zhang[Full Article -
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BRIEF ARTICLES
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3186-3188
Highly Stable C60/Poly(vinylpyrrolidone) Charge-Transfer Complexes Afford New Predictions for Biological Applications of Underivatized Fullerenes
Cezar Ungurenasu and
Anton Airinei[Full Article -
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3189-3192
Synthesis, Characterization, and Cytotoxicity of Trifunctional Dinuclear Platinum Complexes: Comparison of Effects of Geometry and Polyfunctionality on Biological Activity
Yun Qu,
Holger Rauter,
Ana Paula Soares Fontes,
Ramani Bandarage,
Lloyd R. Kelland, and
Nicholas Farrell[Full Article -
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3193-3196
Probes for Narcotic Receptor-Mediated Phenomena. 27. Synthesis and Pharmacological Evaluation of Selective  -Opioid Receptor Agonists from 4-[( R)--(2S,5R)-4-Substituted-2,5-dimethyl-1-piperazinyl-3-methoxybenzyl]- N,N-diethylbenzamides and Their Enantiomers
M. Scott Furness,
Xiaoyan Zhang,
Andrew Coop,
Arthur E. Jacobson,
Richard B. Rothman,
Christina M. Dersch,
Heng Xu,
Frank Porreca, and
Kenner C. Rice[Full Article -
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BOOK REVIEWS
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3197-3198
| Drug Metabolism Databases and High-Throughput Testing During Drug Design and Development Edited by Paul W. Ehrhardt. International Union of Pure and Applied Chemistry, Blackwell Science, Ltd., Malden, MA. 1999. 340 pp. 19 x 25 cm. ISBN 0-632-05342-9. $60.00.
Rory P. Remmel
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ADDITIONS AND CORRECTIONS
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3199-3199
| Tyrosine Kinase Inhibitors. 17. Irreversible Inhibitors of the Epidermal Growth Factor Receptor: 4-(Phenylamino)quinazoline- and 4-(Phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides Bearing Additional Solubilizing Functions.
Jeff B. Smaill,
Gordon W. Rewcastle,
Joseph A. Loo,
Kenneth D. Greis,
O. Helen Chan,
Eric L. Reyner,
Elke Lipka,
H. D. Hollis Showalter,
Patrick W. Vincent,
William L. Elliott, and
William A. Denny:
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3200-3200
| New Anilinophthalazines as Potent and Orally Well Absorbed Inhibitors of the VEGF Receptor Tyrosine Kinases Useful as Antagonists of Tumor-Driven Angiogenesis.
Guido Bold,
Karl-Heinz Altmann,
Jörg Frei,
Marc Lang,
Paul W. Manley,
Peter Traxler,
Bernhard Wietfeld,
Josef Brüggen,
Elisabeth
Buchdunger,
Robert Cozens,
Stefano Ferrari,
Pascal Furet,
Francesco Hofmann,
Georg
Martiny-Baron,
Jürgen Mestan,
Johannes Rösel,
Matthew Sills,
David Stover,
Figan Acemoglu,
Eugen Boss,
René Emmenegger,
Laurent Lässer,
Elvira Masso,
Rosemari Roth,
Christian Schlachter,
Werner Vetterli,
Dominique Wyss, and
Jeanette M. Wood:
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