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3759-3763
Novel Lead Generation through Hypothetical Pharmacophore Three-Dimensional Database Searching: Discovery of Isoflavonoids as Nonsteroidal Inhibitors of Rat 5 -Reductase
Grace Shiahuy Chen,
Chih-Shiang Chang,
Wai Ming Kan,
Chih-Long Chang,
K. C. Wang, and
Ji-Wang Chern
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3764-3767
Design and Synthesis of 4-Substituted Benzamides as Potent, Selective, and Orally Bioavailable IKs Blockers
John Lloyd,
Joan B. Schmidt,
George Rovnyak,
Saleem Ahmad,
Karnail S. Atwal,
Sharon N. Bisaha,
Lidia M. Doweyko,
Philip D. Stein,
Sarah C. Traeger,
Arvind Mathur,
Mary Lee Conder,
John DiMarco,
Timothy W. Harper,
Tonya Jenkins-West,
Paul C. Levesque,
Diane E. Normandin,
Anita D. Russell,
Randolph P. Serafino,
Mark A. Smith, and
Nicholas J. Lodge
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3768-3785
Evaluation of Docking Functions for Protein-Ligand Docking
Carlos Pérez and
Angel R. Ortiz
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3786-3794
Modeling of Poly(ADP-ribose)polymerase (PARP) Inhibitors. Docking of Ligands and Quantitative Structure-Activity Relationship Analysis
Gabriele Costantino,
Antonio Macchiarulo,
Emidio Camaioni, and
Roberto Pellicciari
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3795-3809
One-Dimensional Molecular Representations and Similarity Calculations: Methodology and Validation
Steven L. Dixon and
Kenneth M. Merz, Jr.
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3810-3820
Acetylcholinesterase Inhibitors: SAR and Kinetic Studies on  -[N-Methyl-N-(3-alkylcarbamoyloxyphenyl)methyl]aminoalkoxyaryl Derivatives
Angela Rampa,
Lorna Piazzi,
Federica Belluti,
Silvia Gobbi,
Alessandra Bisi,
Manuela Bartolini,
Vincenza Andrisano,
Vanni Cavrini,
Andrea Cavalli,
Maurizio Recanatini, and
Piero Valenti
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3821-3830
17-O-(Aminoalkyl)oxime Derivatives of 3 ,14-Dihydroxy-5-androstane and 3-Hydroxy-14-oxoseco-D-5-androstane as Inhibitors of Na+,K+-ATPase at the Digitalis Receptor
Mauro Gobbini,
Paolo Barassi,
Alberto Cerri,
Sergio De Munari,
Giorgio Fedrizzi,
Marco Santagostino,
Antonio Schiavone,
Marco Torri, and
Piero Melloni
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3831-3837
Synthesis and Activity of Novel and Selective IKs-Channel Blockers
Uwe Gerlach,
Joachim Brendel,
Hans-Jochen Lang,
Erich F. Paulus,
Klaus Weidmann,
Andrea Brüggemann,
Andreas E. Busch,
Hartmut Suessbrich,
Markus Bleich, and
Rainer Greger
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3838-3848
Synthesis and Biological Evaluation of a Novel Series of Furans: Ligands Selective for Estrogen Receptor
Deborah S. Mortensen,
Alice L. Rodriguez,
Kathryn E. Carlson,
Jun Sun,
Benita S. Katzenellenbogen, and
John A. Katzenellenbogen
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3849-3855
Three-Dimensional Quantitative Structure-Activity Relationship (3D-QSAR) Models for a Novel Class of Piperazine-Based Stromelysin-1 (MMP-3) Inhibitors: Applying a "Divide and Conquer" Strategy
Elizabeth Ambrose Amin and
William J. Welsh
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3856-3871
Exploiting Subsite S1 of Trypsin-Like Serine Proteases for Selectivity: Potent and Selective Inhibitors of Urokinase-Type Plasminogen Activator
Richard L. Mackman,
Bradley A. Katz,
J. Guy Breitenbucher,
Hon C. Hui,
Erik Verner,
Christine Luong,
Liang Liu, and
Paul A. Sprengeler
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3872-3880
Iridals Are a Novel Class of Ligands for Phorbol Ester Receptors with Modest Selectivity for the RasGRP Receptor Subfamily
Lei Shao,
Nancy E. Lewin,
Patricia S. Lorenzo,
Zengjian Hu,
Istvan J. Enyedy,
Susan H. Garfield,
James C. Stone,
Franz-Josef Marner,
Peter M. Blumberg, and
Shaomeng Wang
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3881-3895
N-Arylsulfonylindole Derivatives as Serotonin 5-HT6 Receptor Ligands
Michael G. N. Russell,
Robert J. Baker,
Laura Barden,
Margaret S. Beer,
Linda Bristow,
Howard B. Broughton,
Michael Knowles,
George McAllister,
Smita Patel, and
José L. Castro
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3896-3903
Pseudoproline-Containing Analogues of Morphiceptin and Endomorphin-2: Evidence for a Cis Tyr-Pro Amide Bond in the Bioactive Conformation
Michael Keller,
Christophe Boissard,
Luc Patiny,
Nga N. Chung,
Carole Lemieux,
Manfred Mutter, and
Peter W. Schiller
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3904-3914
A Novel Series of 2,6,7-Substituted 2,3-Dihydro-1,4-Benzodioxin and 2,6,7-Substituted 1,4-Benzodioxin Derivatives as Lipid Peroxidation Inhibitors. Structure-Activity Relationships for High Inhibition of Human Low-Density Lipoprotein Peroxidation
Valérie Thiéry,
Gérard Coudert,
Jean-Guy Bizot-Espiard,
Bruno Pfeiffer,
Pierre Renard,
Albert Lindenbaum, and
Gérald Guillaumet
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3915-3924
Preparation and Evaluation of Sulfide Derivatives of the Antibiotic Brefeldin A as Potential Prodrug Candidates with Enhanced Aqueous Solubilities
Brian M. Fox,
Jeffrey A. Vroman,
Phillip E. Fanwick, and
Mark Cushman
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3925-3931
Phenoxypropoxybiguanides, Prodrugs of DHFR-Inhibiting Diaminotriazine Antimalarials
Norman P. Jensen,
Arba L. Ager,
Robert A. Bliss,
Craig J. Canfield,
Barbara M. Kotecka,
Karl H. Rieckmann,
Jacek Terpinski, and
David P. Jacobus
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3932-3936
Antitumor Agents. 211. Fluorinated 2-Phenyl-4-quinolone Derivatives as Antimitotic Antitumor Agents
Yi Xia,
Zheng-Yu Yang,
Peng Xia,
Torben Hackl,
Ernest Hamel,
Anthony Mauger,
Jiu-Hong Wu, and
Kuo-Hsiung Lee
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3937-3945
Synthesis and Biological Evaluation of Tropane-like 1-{2-[Bis(4-fluorophenyl)methoxy]ethyl}-4-(3-phenylpropyl)piperazine (GBR 12909) Analogues
Ying Zhang,
David B. Joseph,
Wayne D. Bowen,
Judith L. Flippen-Anderson,
Christina M. Dersch,
Richard B. Rothman,
Arthur E. Jacobson, and
Kenner C. Rice
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3946-3955
Structure-Affinity Relationships of a Unique Nicotinic Ligand: N-Dimethyl-N4-phenylpiperazinium Iodide (DMPP)
Maria Novella Romanelli,
Dina Manetti,
Serena Scapecchi,
Pier Andrea Borea,
Silvia Dei,
Alessandro Bartolini,
Carla Ghelardini,
Fulvio Gualtieri,
Luca Guandalini, and
Katia Varani
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3956-3964
Structure-Activity Studies of the Phe4 Residue of Nociceptin(1-13)-NH2: Identification of Highly Potent Agonists of the Nociceptin/Orphanin FQ Receptor
Remo Guerrini,
Girolamo Caló,
Raffaella Bigoni,
Daniela Rizzi,
Anna Rizzi,
Marina Zucchini,
Katia Varani,
Eiji Hashiba,
David G. Lambert,
Geza Toth,
Pier Andrea Borea,
Severo Salvadori, and
Domenico Regoli
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3965-3977
Optimization of 4-Phenylamino-3-quinolinecarbonitriles as Potent Inhibitors of Src Kinase Activity
Diane H. Boschelli,
Fei Ye,
Yanong D. Wang,
Minu Dutia,
Steve L. Johnson,
Biqi Wu,
Karen Miller,
Dennis W. Powell,
Deanna Yaczko,
Mairead Young,
Mark Tischler,
Kim Arndt,
Carolyn Discafani,
Carlo Etienne,
Jay Gibbons,
Janet Grod,
Judy Lucas,
Jennifer M. Weber, and
Frank Boschelli
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3978-3984
Pyrrolidine-3-carboxylic Acids as Endothelin Antagonists. 5. Highly Selective, Potent, and Orally Active ETA Antagonists
Hwan-Soo Jae,
Martin Winn,
Thomas W. von Geldern,
Bryan K. Sorensen,
William J. Chiou,
Bach Nguyen,
Kennan C. Marsh, and
Terry J. Opgenorth
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3985-3993
Enantiomeric Synthesis of D- and L-Cyclopentenyl Nucleosides and Their Antiviral Activity Against HIV and West Nile Virus
Gyu Y. Song,
Vincent Paul,
Hyunah Choo,
John Morrey,
Robert W. Sidwell,
Raymond F. Schinazi, and
Chung K. Chu
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3994-4000
Design, Synthesis, and Characterization of the Antitumor Activity of Novel Ceramide Analogues
Marco Macchia,
Silvia Barontini,
Simone Bertini,
Valeria Di Bussolo,
Stefano Fogli,
Elisa Giovannetti,
Enzo Grossi,
Filippo Minutolo, and
Romano Danesi
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4001-4010
Discovery of a Series of Nonpeptide Small Molecules That Inhibit the Binding of Insulin-like Growth Factor (IGF) to IGF-Binding Proteins
Chen Chen,
Yun-Fei Zhu,
Xin-Jun Liu,
Zi-Xian Lu,
Qiu Xie, and
Nicholas Ling
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4011-4014
Synthesis and Screening for Antiacetylcholinesterase Activity of (1-Benzyl-4-oxopiperidin-3-ylidene)methylindoles and -pyrroles Related to Donepezil
Aldo Andreani,
Andrea Cavalli,
Massimiliano Granaiola,
Massimo Guardigli,
Alberto Leoni,
Alessandra Locatelli,
Rita Morigi,
Mirella Rambaldi,
Maurizio Recanatini, and
Aldo Roda
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4015-4018
Structure-Activity Studies on Nociceptin Analogues: ORL1 Receptor Binding and Biological Activity of Cyclic Disulfide-Containing Analogues of Nociceptin Peptides
Akihiro Ambo,
Naohumi Hamazaki,
Yoshinari Yamada,
Eriko Nakata, and
Yusuke Sasaki
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4019-4022
Methylene-gem-Difluorocyclopropane Analogues of Nucleosides: Synthesis, Cyclopropene-Methylenecyclopropane Rearrangement, and Biological Activity
Ruifang Wang,
Mohamad B. Ksebati,
Thomas H. Corbett,
Earl R. Kern,
John C. Drach, and
Jiri Zemlicka
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4023-4026
New Pyridoquinoline Derivatives as Potential Inhibitors of the Fluoroquinolone Efflux Pump in Resistant Enterobacter aerogenes Strains
Jacqueline Chevalier,
Siham Atifi,
Annie Eyraud,
Abdallah Mahamoud,
Jacques Barbe, and
Jean-Marie Pagès
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