3141-3143
| Synthesis and Pharmacological Characterization of 3-[2-((3aR,9bR)-cis-6-Methoxy- 2,3,3a,4,5,9b-hexahydro-1H- benz[e]isoindol-2-yl)ethyl]pyrido[3',4':4,5]thieno[3,2-d]pyrimidine- 2,4(1H,3H)-dione (A-131701): A Uroselective  1A Adrenoceptor Antagonist for the Symptomatic Treatment of Benign Prostatic Hyperplasia
Michael D. Meyer,
Robert J. Altenbach,
Fatima Z. Basha,
William A. Carroll,
Irene Drizin,
Steven W. Elmore,
Paul P. Ehrlich,
Suzanne A. Lebold,
Karin Tietje,
Kevin B. Sippy,
Michael D. Wendt,
Daniel J. Plata,
Fred Plagge,
Steven A. Buckner,
Michael E. Brune,
Arthur A. Hancock, and
James F. Kerwin, Jr.
[Full Article -
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3144-3150
| NMR-Based Discovery of Lead Inhibitors That Block DNA Binding of the Human Papillomavirus E2 Protein
Philip J. Hajduk,
Jürgen Dinges,
Gregory F. Miknis,
Megan Merlock,
Tim Middleton,
Dale J. Kempf,
David A. Egan,
Karl A. Walter,
Terry S. Robins,
Suzy B. Shuker,
Thomas F. Holzman, and
Stephen W. Fesik
[Full Article -
PDF] |
3151-3160
| Synthesis and Evaluation of Novel Rhodacyanine Dyes That Exhibit Antitumor Activity
Masayuki Kawakami,
Keizo Koya,
Toshinao Ukai,
Noriaki Tatsuta,
Akihiko Ikegawa,
Keizo Ogawa,
Tadao Shishido, and
Lan Bo Chen
[Full Article -
PDF] |
3161-3172
| Validation of EGSITE2, a Mixed Integer Program for Deducing Objective Site Models from Experimental Binding Data
Gordon M. Crippen
[Full Article -
PDF] |
3173-3181
| Orally Active Trifluoromethyl Ketone Inhibitors of Human Leukocyte Elastase
Chris A. Veale,
Peter R. Bernstein,
Claudia M. Bohnert,
Frederick J. Brown,
Craig Bryant,
James R. Damewood, Jr.,
Roger Earley,
Scott W. Feeney,
Philip D. Edwards,
Bruce Gomes,
James M. Hulsizer,
Ben J. Kosmider,
Robert D. Krell,
Gary Moore,
Theodora W. Salcedo,
Andrew Shaw,
David S. Silberstein,
Gary B. Steelman,
Mark Stein,
Anne Strimpler,
Roy M. Thomas,
Edward P. Vacek,
Joseph C. Williams,
Donald J. Wolanin, and
Sheila Woolson
[Full Article -
PDF] |
3182-3191
| Structure-Activity Studies for -Amino-3-hydroxy-5-methyl-4-isoxazolepropanoic Acid Receptors: Acidic Hydroxyphenylalanines
Ronald A. Hill,
Lane J. Wallace,
Duane D. Miller,
David M. Weinstein,
Gamal Shams,
Henry Tai,
Richard T. Layer,
David Willins,
Norman J. Uretsky, and
Satyavijayan Narasimhan Danthi
[Full Article -
PDF] |
3192-3198
| Discovery of a Novel Class of Substituted Pyrrolooctahydroisoquinolines as Potent and Selective  Opioid Agonists, Based on an Extension of the Message-Address Concept
Giulio Dondio,
Silvano Ronzoni,
Drake S. Eggleston,
Marco Artico,
Paola Petrillo,
Giuseppe Petrone,
Luciano Visentin,
Carlo Farina,
Vittorio Vecchietti, and
Geoffrey D. Clarke
[Full Article -
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3199-3206
| A Model for Binding of Structurally Diverse Natural Product Inhibitors of Protein Phosphatases PP1 and PP2A
Varsha Gupta,
Anthony K. Ogawa,
Xiaohui Du,
K. N. Houk, and
Robert W. Armstrong
[Full Article -
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3207-3216
| 6-(Alkylamino)-9-alkylpurines. A New Class of Potential Antipsychotic Agents
James L. Kelley,
R. Morris Bullock,
Mark P. Krochmal,
Ed W. McLean,
James A. Linn,
Micheal J. Durcan, and
Barrett R. Cooper
[Full Article -
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3217-3227
| Pyrrolidine-3-carboxylic Acids as Endothelin Antagonists. 2. Sulfonamide-Based ETA/ETB Mixed Antagonists
Hwan-Soo Jae,
Martin Winn,
Douglas B. Dixon,
Kennan C. Marsh,
Bach Nguyen,
Terry J. Opgenorth, and
Thomas W. von Geldern
[Full Article -
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3228-3233
| Cannabinol Derivatives: Binding to Cannabinoid Receptors and Inhibition of Adenylylcyclase
Man-Hee Rhee,
Zvi Vogel,
Jacob Barg,
Michael Bayewitch,
Rivka Levy,
Lumir Hanu,
Aviva Breuer, and
Raphael Mechoulam
[Full Article -
PDF] |
3234-3247
| Sulfated Galactocerebrosides as Potential Antiinflammatory Agents
Anne Marinier,
Alain Martel,
Jacques Banville,
Carol Bachand,
Roger Remillard,
Philippe Lapointe,
Brigitte Turmel,
Marcel Menard,
William E. Harte, Jr.,
J. J. Kim Wright,
Gordon Todderud,
Kenneth M. Tramposch,
Jürgen Bajorath,
Diane Hollenbaugh, and
Alejandro Aruffo
[Full Article -
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3248-3253
| Selective Inhibitors of Cyclic AMP-Specific Phosphodiesterase: Heterocycle-Condensed Purines
Hiroyuki Sawanishi,
Hirokazu Suzuki,
Shinya Yamamoto,
Yoshihiro Waki,
Shohei Kasugai,
Keiichi Ohya,
Nagao Suzuki,
Ken-ichi Miyamoto, and
Kenzo Takagi
[Full Article -
PDF] |
3254-3262
| Molecular Simulation of Dynorphin A-(1-10) Binding to Extracellular Loop 2 of the  -Opioid Receptor. A Model for Receptor Activation
Germana Paterlini,
Philip S. Portoghese, and
David M. Ferguson
[Full Article -
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3263-3270
| 6 -Propynyl-Substituted Steroids: Mechanism-Based Enzyme-Activated Irreversible Inhibitors of Aromatase
Abraham Akkani,
Germana Paterlini,
William B. Gleason,
William H. Ojala, and
Yusuf J. Abul-Hajj
[Full Article -
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3271-3279
| Angiotensin Analogues Palmitoylated in Positions 1 and 4
Lenka Maletínská,
Witold Neugebauer,
Jacqueline Pérodin,
Marie Lefebvre, and
Emanuel Escher
[Full Article -
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3280-3291
| Synthesis and Evaluation of Novel Fluorinated Methotrexate Derivatives for Application to Rheumatoid Arthritis Treatment
Yoshitsugu Kokuryo,
Kyozo Kawata,
Takuji Nakatani,
Akira Kugimiya,
Yoshinori Tamura,
Kenji Kawada,
Mitsunobu Matsumoto,
Ryuji Suzuki,
Kenji Kuwabara,
Yozo Hori, and
Mitsuaki Ohtani
[Full Article -
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3292-3296
| DNA Gyrase Inhibitory and Antimicrobial Activities of Some Diphenic Acid Monohydroxamides
Kwasi A. Ohemeng,
Brent L. Podlogar,
Van N. Nguyen,
Jeffrey I. Bernstein,
Heather M. Krause,
Jamese J. Hilliard, and
John F. Barrett
[Full Article -
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3297-3304
| 17-Imidazolyl, Pyrazolyl, and Isoxazolyl Androstene Derivatives. Novel Steroidal Inhibitors of Human Cytochrome Cl7,20-Lyase (P45017)
Yang-zhi Ling,
Ji-song Li,
Yang Liu,
Katsuya Kato,
Gregory T. Klus, and
Angela Brodie
[Full Article -
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3305-3311
| Conformational Studies of Paclitaxel Analogs Modified at the C-2' Position in Hydrophobic and Hydrophilic Solvent Systems
Guillermo Moyna,
Howard J. Williams, and
A. I. Scott
, Israel Ringel and
Raphael Gorodetsky
, Charles S. Swindell
[Full Article - PDF] |
3312-3318
| Importance of the C-1 Substituent in Classical Cannabinoids to CB2 Receptor Selectivity: Synthesis and Characterization of a Series of O,2-Propano- 8-tetrahydrocannabinol Analogs
Patricia H. Reggio,
Tiansheng Wang,
Amy E. Brown,
Denise N. Fleming,
Herbert H. Seltzman,
Graeme Griffin,
Roger G. Pertwee,
David R. Compton,
Mary E. Abood, and
Billy R. Martin
[Full Article - PDF] |