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2861-2864
Specific Inhibition of a Family 1A Dihydroorotate Dehydrogenase by Benzoate Pyrimidine Analogues
Bruce A. Palfey,
Olof Björnberg, and
Kaj Frank Jensen
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2865-2868
Structure-Based Design: Potent Inhibitors of Human Brain Memapsin 2 ( -Secretase)
Arun K. Ghosh,
Geoffrey Bilcer,
Cynthia Harwood,
Reiko Kawahama,
Dongwoo Shin,
Khaja Azhar Hussain,
Lin Hong,
Jeffrey A. Loy,
Chan Nguyen,
Gerald Koelsch,
Jacques Ermolieff, and
Jordan Tang
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2869-2878
Utilization of a Peptide Lead for the Discovery of a Novel PTP1B-Binding Motif
Yang Gao,
Johannes Voigt,
He Zhao,
Godwin C. G. Pais,
Xuechun Zhang,
Li Wu,
Zhong-Yin Zhang, and
Terrence R. Burke, Jr.
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2879-2885
Synthesis and Characterization of Non-Steroidal Ligands for the Glucocorticoid Receptor: Selective Quinoline Derivatives with Prednisolone-Equivalent Functional Activity
Michael J. Coghlan,
Philip R. Kym,
Steven W. Elmore,
Alan X. Wang,
Jay R. Luly,
Denise Wilcox,
Michael Stashko,
Chun-Wei Lin,
Jeffrey Miner,
Curtis Tyree,
Masaki Nakane,
Peer Jacobson, and
Benjamin C. Lane
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2886-2899
Synthesis, Molecular Modeling, and Structure-Activity Relationship of Benzophenone-Based CAAX-Peptidomimetic Farnesyltransferase Inhibitors
Jacek Sakowski,
Markus Böhm,
Isabel Sattler,
Hans-Martin Dahse, and
Martin Schlitzer
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2900-2912
2-N-Acylaminoalkylindoles: Design and Quantitative Structure-Activity Relationship Studies Leading to MT2-Selective Melatonin Antagonists
Gilberto Spadoni,
Cesarino Balsamini,
Giuseppe Diamantini,
Andrea Tontini, and
Giorgio Tarzia
, Marco Mor,
Silvia Rivara, and
Pier Vincenzo Plazzi
, Romolo Nonno,
Valeria Lucini,
Marilou Pannacci,
Franco Fraschini, and
Bojidar Michaylov Stankov
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2913-2920
Discovery of Potent Antagonists of Leukocyte Function-Associated Antigen-1/Intercellular Adhesion Molecule-1 Interaction. 3. Amide (C-Ring) Structure-Activity Relationship and Improvement of Overall Properties of Arylthio Cinnamides
Zhonghua Pei,
Zhili Xin,
Gang Liu,
Yihong Li,
Edward B. Reilly,
Nathan L. Lubbers,
Jeffery R. Huth,
James T. Link,
Thomas W. von Geldern,
Bryan F. Cox,
Sandra Leitza,
Yi Gao,
Kennan C. Marsh,
Peter DeVries, and
Greg F. Okasinski
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2921-2927
Design and Synthesis of 4,5-Diphenyl-4-isoxazolines: Novel Inhibitors of Cyclooxygenase-2 with Analgesic and Antiinflammatory Activity
Amgad G. Habeeb,
P. N. Praveen Rao, and
Edward E. Knaus
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2928-2932
X-ray Crystal Structures of Candida albicans Dihydrofolate Reductase: High Resolution Ternary Complexes in Which the Dihydronicotinamide Moiety of NADPH Is Displaced by an Inhibitor
Marc Whitlow,
Andrew J. Howard,
David Stewart,
Karl D. Hardman,
Joseph H. Chan,
David P. Baccanari,
Robert L. Tansik,
Jean S. Hong, and
Lee F. Kuyper
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2933-2949
Design and Biological Activity of (S)-4-(5-{[1-(3-Chlorobenzyl)-2- oxopyrrolidin-3-ylamino]methyl}imidazol-1-ylmethyl)benzonitrile, a 3-Aminopyrrolidinone Farnesyltransferase Inhibitor with Excellent Cell Potency
Ian M. Bell,
Steven N. Gallicchio,
Marc Abrams,
Douglas C. Beshore,
Carolyn A. Buser,
J. Christopher Culberson,
Joseph Davide,
Michelle Ellis-Hutchings,
Christine Fernandes,
Jackson B. Gibbs,
Samuel L. Graham,
George D. Hartman,
David C. Heimbrook,
Carl F. Homnick,
Joel R. Huff,
Kelem Kassahun,
Kenneth S. Koblan,
Nancy E. Kohl,
Robert B. Lobell,
Joseph J. Lynch, Jr,
Patricia A. Miller,
Charles A. Omer,
A. David Rodrigues,
Eileen S. Walsh, and
Theresa M. Williams
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2950-2958
Novel Hypotensive Agents from Verbesina caracasana. 8. Synthesis and Pharmacology of (3,4-Dimethoxycinnamoyl)-N-agmatine and Synthetic Analogues1
Marco Carmignani,
Anna Rita Volpe,
Bruno Botta,
Romulo Espinal,
Stella C. De Bonnevaux,
Carlo De Luca,
Maurizio Botta,
Federico Corelli,
Andrea Tafi,
Rosario Sacco, and
Giuliano Delle Monache
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2959-2965
Synthesis and in Vitro Antitumor Activity of Oligonucleotide-Tethered and Related Platinum Complexes
Lisheng Cai,
Keunpoong Lim,
Sumei Ren,
Rhonda S. Cadena, and
William T. Beck
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2966-2975
5'-O-Alkyl Ethers of N,2-Substituted Adenosine Derivatives: Partial Agonists for the Adenosine A1 and A3 Receptors
Erica W. van Tilburg,
Pieter A. M. van der Klein,
Jacobien von Frijtag Drabbe Künzel,
Miriam de Groote,
Christina Stannek,
Anna Lorenzen, and
Ad P. IJzerman
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2976-2983
QSAR Study on the Contribution of Log P and Es to the in Vitro Antiprotozoal Activity of Glutathione Derivatives
Sylvie Daunes and
Claudius D'Silva
, Howard Kendrick,
Vanessa Yardley, and
Simon L. Croft
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2984-2989
Synthesis and Biological Activity of D- and L-chiro-Inositol 2,3,4,5-Tetrakisphosphate: Design of a Novel and Potent Inhibitor of Ins(3,4,5,6)P4 1-Kinase/Ins(1,3,4)P3 5/6-Kinase
Changsheng Liu,
Andrew M. Riley,
Xiaonian Yang,
Stephen B. Shears, and
Barry V. L. Potter
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2990-3000
Identification of Potent Non-Peptide Somatostatin Antagonists with sst3 Selectivity
Lydie Poitout,
Pierre Roubert,
Marie-Odile Contour-Galcéra,
Christophe Moinet,
Jacques Lannoy,
Jacques Pommier,
Pascale Plas,
Dennis Bigg, and
Christophe Thurieau
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3001-3013
Novel Azo Derivatives as Prodrugs of 5-Aminosalicylic Acid and Amino Derivatives with Potent Platelet Activating Factor Antagonist Activity
Elena Carceller,
Jordi Salas,
Manuel Merlos,
Marta Giral,
Rosa Ferrando,
Ignasi Escamilla,
Joaquin Ramis,
Julián García-Rafanell, and
Javier Forn
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3014-3021
New 3'-Azido-3'-deoxythymidin-5'-yl O-(4-Hydroxyalkyl or -Alkenyl or -Alkylepoxide) Carbonate Prodrugs: Synthesis and Anti-HIV Evaluation
Patrick Vlieghe,
Thierry Clerc,
Christophe Pannecouque,
Myriam Witvrouw,
Erik De Clercq,
Jean-Pierre Salles, and
Jean-Louis Kraus
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3022-3030
Design, Synthesis and Pharmacological Characterization of a Potent Radioiodinated and Photoactivatable Peptidic Oxytocin Antagonist
Eric Carnazzi,
André Aumelas,
Bernard Mouillac,
Christophe Breton,
Laurent Guillou,
Claude Barberis, and
René Seyer
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3031-3038
S(+)-4-(1-Phenylethylamino)quinazolines as Inhibitors of Human Immunoglobuline E Synthesis: Potency Is Dictated by Stereochemistry and Atomic Point Charges at N-1
Michael Berger,
Bettina Albrecht,
Attila Berces,
Peter Ettmayer,
Wolfgang Neruda, and
Maximilian Woisetschläger
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3039-3042
Design and Synthesis of Celecoxib and Rofecoxib Analogues as Selective Cyclooxygenase-2 (COX-2) Inhibitors: Replacement of Sulfonamide and Methylsulfonyl Pharmacophores by an Azido Bioisostere
Amgad G. Habeeb,
P. N. Praveen Rao, and
Edward E. Knaus
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