2063-2063
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ANNOUNCEMENTS
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ARTICLES
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2064-2086
Structure-Antiviral Activity Relationship in the Series of Pyrimidine and Purine N-[2-(2-Phosphonomethoxy)ethyl] Nucleotide Analogues. 1. Derivatives Substituted at the Carbon Atoms of the Base
Antonín Hol,
Jaroslav Günter,
Hana Dvoáková,
Milena Masojídková,
Graciela Andrei,
Robert Snoeck,
Jan Balzarini, and
Erik De Clercq
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2087-2104
Fluorination of 3-(3-(Piperidin-1-yl)propyl)indoles and 3-(3-(Piperazin-1-yl)propyl)indoles Gives Selective Human 5-HT1D Receptor Ligands with Improved Pharmacokinetic Profiles
Monique B. van Niel,
Ian Collins,
Margaret S. Beer,
Howard B. Broughton,
Susan K. F. Cheng,
Simon C. Goodacre,
Anne Heald,
Karen L. Locker,
Angus M. MacLeod,
Denise Morrison,
Christopher R. Moyes,
Desmond O'Connor,
Andrew Pike,
Michael Rowley,
Michael G. N. Russell,
Balbinder Sohal,
Josephine A. Stanton,
Steven Thomas,
Hugh Verrier,
Alan P. Watt, and
José L. Castro
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2105-2111
A Peptide Agonist Acts by Occupation of a Monomeric G Protein-Coupled Receptor: Dual Sites of Covalent Attachment to Domains Near TM1 and TM7 of the Same Molecule Make Biologically Significant Domain-Swapped Dimerization Unlikely
Elizabeth M. Hadac,
Zongshi Ji,
Delia I. Pinon,
Randal M. Henne,
Terry P. Lybrand, and
Laurence J. Miller
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2112-2124
Phthalein Derivatives as a New Tool for Selectivity in Thymidylate Synthase Inhibition
Paola M. Costi,
Marcella Rinaldi,
Donatella Tondi,
Piergiorgio Pecorari,
Daniela Barlocco,
Stefano Ghelli,
Robert M. Stroud,
Daniel V. Santi,
Thomas J. Stout,
Chiara Musiu,
Elena M. Marangiu,
Alessandra Pani,
Donatella Congiu,
Giulia A. Loi, and
Paolo La Colla
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2125-2135
Tricyclic Farnesyl Protein Transferase Inhibitors: Crystallographic and Calorimetric Studies of Structure-Activity Relationships
Corey L. Strickland,
Patricia C. Weber,
William T. Windsor,
Zhen Wu,
Hung V. Le,
Margaret M. Albanese,
Carmen S. Alvarez,
David Cesarz,
Joycelyn del Rosario,
Jeffrey Deskus,
Alan K. Mallams,
F. George Njoroge,
John J. Piwinski,
Stacy Remiszewski,
Randall R. Rossman,
Arthur G. Taveras,
Bancha Vibulbhan,
Ronald J. Doll,
Viyyoor M. Girijavallabhan, and
Ashit K. Ganguly
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2136-2144
Design and Synthesis of Modified Quinolones as Antitumoral Acridones
Oriana Tabarrini,
Violetta Cecchetti,
Arnaldo Fravolini,
Giuseppe Nocentini,
A. Barzi,
Stefano Sabatini,
Hua Miao, and
Claudia Sissi
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2145-2161
Novel Multidrug Resistance Reversal Agents
Dan Berger,
Ron Citarella,
Minu Dutia,
Lee Greenberger,
William Hallett,
Rolf Paul, and
Dennis Powell
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2162-2168
Butenolide Endothelin Antagonists with Improved Aqueous Solubility
William C. Patt,
Xue-Min Cheng,
Joseph T. Repine,
Chet Lee,
Bill R. Reisdorph,
Mark A. Massa,
Annette M. Doherty,
Kathleen M. Welch,
John W. Bryant,
Michael A. Flynn,
Donnelle M. Walker,
Richard L. Schroeder,
Stephen J. Haleen, and
Joan A. Keiser
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2169-2179
Prediction of Ligand-Receptor Binding Thermodynamics by Free Energy Force Field Three-Dimensional Quantitative Structure-Activity Relationship Analysis: Applications to a Set of Glucose Analogue Inhibitors of Glycogen Phosphorylase
Prabha Venkatarangan and
Anton J. Hopfinger
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2180-2190
Design and Synthesis of Potent, Selective, and Orally Bioavailable Tetrasubstituted Imidazole Inhibitors of p38 Mitogen-Activated Protein Kinase
Nigel J. Liverton,
John W. Butcher,
Christopher F. Claiborne,
David A. Claremon,
Brian E. Libby,
Kevin T. Nguyen,
Steven M. Pitzenberger,
Harold G. Selnick,
Garry R. Smith,
Andrew Tebben,
Joseph P. Vacca,
Sandor L. Varga,
Lily Agarwal,
Kim Dancheck,
Amy J. Forsyth,
Daniel S. Fletcher,
Betsy Frantz,
William A. Hanlon,
Coral F. Harper,
Scott J. Hofsess,
Matthew Kostura,
Jiunn Lin,
Sylvie Luell,
Edward A. O'Neill,
Chad J. Orevillo,
Margaret Pang,
Janey Parsons,
Anna Rolando,
Yousif Sahly,
Denise M. Visco, and
Stephen J. O'Keefe
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2191-2203
Synthesis of 9-O-Substituted Derivatives of 9-Hydroxy-5,6-dimethyl-6H- pyrido[4,3-b]carbazole-1-carboxylic Acid (2-(Dimethylamino)ethyl)amide and Their 10- and 11-Methyl Analogues with Improved Antitumor Activity
Claude Guillonneau,
Alain Pierré,
Yves Charton,
Nicolas Guilbaud,
Laurence Kraus-Berthier,
Stéphane Léonce,
André Michel,
Emile Bisagni, and
Ghanem Atassi
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2204-2211
Stereoselective Characterization of the 1,4-Dihydropyridine Binding Site at L-Type Calcium Channels in the Resting State and the Opened/Inactivated State
Klaus-Jürgen Schleifer
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2212-2217
Structure-Activity Relationships of L-Dioxolane Uracil Nucleosides as Anti-Epstein Barr Virus Agents
Ju-Sheng Lin,
Toshihiko Kira,
Elizabeth Gullen,
Yongseok Choi,
Fucheng Qu,
Chung K. Chu, and
Yung-Chi Cheng
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2218-2226
Benzodiazepine Receptor Ligands. 4. Synthesis and Pharmacological Evaluation of 3-Heteroaryl-8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-Oxides
Annarella Costanzo,
Gabriella Guerrini,
Giovanna Ciciani,
Fabrizio Bruni,
Silvia Selleri,
Barbara Costa,
Claudia Martini,
Antonio Lucacchini,
Petra Malmberg Aiello, and
Alessandra Ipponi
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2227-2234
Novel and Potent 6-Chloro-3-pyridinyl Ligands for the 42 Neuronal Nicotinic Acetylcholine Receptor
Bachir Latli,
Kevin D'Amour, and
John E. Casida
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2235-2244
New (Sulfonyloxy)piperazinyldibenzazepines as Potential Atypical Antipsychotics: Chemistry and Pharmacological Evaluation
Yi Liao,
Bastiaan J. Venhuis,
Nienke Rodenhuis,
Wia Timmerman, and
Håkan Wikström
, Eddie Meier
, Gerd D. Bartoszyk,
Henning Böttcher, and
Christoph A. Seyfried
, Staffan Sundell
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2245-2250
Cross-Linking and Sequence-Specific Alkylation of DNA by Aziridinylquinones. 3. Effects of Alkyl Substituents
Robert H. J. Hargreaves,
C. Caroline O'Hare,
John A. Hartley,
David Ross, and
John Butler
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2251-2259
Synthesis and Nicotinic Acetylcholine Receptor in Vivo Binding Properties of 2-Fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: A New Positron Emission Tomography Ligand for Nicotinic Receptors
Frédéric Dollé,
Lilian Dolci,
Héric Valette,
Françoise Hinnen,
Françoise Vaufrey,
Ilonka Guenther,
Chantal Fuseau,
Christine Coulon,
Michel Bottlaender, and
Christian Crouzel
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2260-2265
2,4-Diphenyl Furan Diamidines as Novel Anti-Pneumocystis carinii Pneumonia Agents
Iris Francesconi,
W. David Wilson,
Farial A. Tanious,
James E. Hall,
Brendan C. Bender,
Richard R. Tidwell,
Donald McCurdy, and
David W. Boykin
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BRIEF ARTICLES
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2266-2271
Design and Synthesis of Novel Quinoxaline-2,3-dione AMPA/GlyN Receptor Antagonists: Amino Acid Derivatives
Sham S. Nikam,
John J. Cordon,
Daniel F. Ortwine,
Tycho H. Heimbach,
Anthony C. Blackburn,
Mark G. Vartanian,
Carrie B. Nelson,
Roy D. Schwarz,
Peter A. Boxer, and
Michael F. Rafferty
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2272-2279
Synthesis of Classical and a Nonclassical 2-Amino-4-oxo-6-methyl-5-substituted Pyrrolo[2,3-d]pyrimidine Antifolate Inhibitors of Thymidylate Synthase
Aleem Gangjee,,
Farahnaz Mavandadi,,
Roy L. Kisliuk, and
Sherry F. Queener
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2280-2286
Potent Inhibition of Steroid Sulfatase Activity by 3-O-Sulfamate 17-Benzyl(or 4'-tert-butylbenzyl)estra-1,3,5(10)-trienes: Combination of Two Substituents at Positions C3 and C17 of Estradiol
Liviu C. Ciobanu,
Roch P. Boivin,
Van Luu-The,
Fernand Labrie, and
Donald Poirier
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2287-2294
2-Amino-4-benzyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridines: Novel Selective 3-Adrenoceptor Agonists
Weiping Zheng,
Victor I. Nikulin,
Anish A. Konkar,
Sandeep S. Vansal,
Gamal Shams,
Dennis R. Feller, and
Duane D. Miller
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