COMMUNICATIONS
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4041-4044
Discovery of Potent Cyclic Pseudopeptide Human Tachykinin NK-2 Receptor Antagonists
Danilo Giannotti,
Enzo Perrotta,
Cristina Di Bugno,
Rossano Nannicini,
Nicholas J. S. Harmat,
Alessandro Giolitti,
Riccardo Patacchini,
Anna Rita Renzetti,
Luigi Rotondaro,
Sandro Giuliani,
Maria Altamura, and
Carlo A. Maggi
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EXPEDITED ARTICLES
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4045-4050
(-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a Conformationally Restricted Analogue of Acetylcholine, Is a Highly Selective Full Agonist at the 7 Nicotinic Acetylcholine Receptor
George Mullen,
James Napier,
Michael Balestra,
Thomas DeCory,
Gregory Hale,
John Macor,
Robert Mack,
James Loch III,
Ed Wu,
Alexander Kover,
Patrick Verhoest,
Anthony Sampognaro,
Eifion Phillips,
Yanyi Zhu,
Robert Murray,
Ronald Griffith,
James Blosser,
David Gurley,
Anthony Machulskis,
John Zongrone,
Alan Rosen, and
Jack Gordon
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ARTICLES
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4051-4062
Synthesis of Phenalene and Acenaphthene Derivatives as New Conformationally Restricted Ligands for Melatonin Receptors
Carole Jellimann,
Monique Mathé-Allainmat,
Jean Andrieux,
Stéphane Kloubert,
Jean A. Boutin,
Jean-Paul Nicolas,
Caroline Bennejean,
Philippe Delagrange, and
Michel Langlois
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4063-4070
Rational Design, Synthesis, and Biological Activity of Benzoxazinones as Novel Factor Xa Inhibitors
Danette A. Dudley,
Amy M. Bunker,
Liguo Chi,
Wayne L. Cody,
Debra R. Holland,
Diane P. Ignasiak,
Nancy Janiczek-Dolphin,
Thomas B. McClanahan,
Thomas E. Mertz,
Lakshmi S. Narasimhan,
Stephen T. Rapundalo,
Julia A. Trautschold,
Chad A. Van Huis, and
Jeremy J. Edmunds
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4071-4083
Resistance-Modifying Agents. 8. Inhibition of O6-Alkylguanine-DNA Alkyltransferase by O6-Alkenyl-, O6-Cycloalkenyl-, and O6-(2-Oxoalkyl)guanines and Potentiation of Temozolomide Cytotoxicity in Vitro by O6-(1-Cyclopentenylmethyl)guanine
Roger J. Griffin,
Christine E. Arris,
Christine Bleasdale,
F. Thomas Boyle,
A. Hilary Calvert,
Nicola J. Curtin,
Christine Dalby,
Sreenivas Kanugula,
Nicola K. Lembicz,
David R. Newell,
Anthony E. Pegg, and
Bernard T. Golding
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4084-4097
Resistance-Modifying Agents. 9. Synthesis and Biological Properties of Benzimidazole Inhibitors of the DNA Repair Enzyme Poly(ADP-ribose) Polymerase
Alex W. White,
Robert Almassy,
A. Hilary Calvert,
Nicola J. Curtin,
Roger J. Griffin,
Zdenek Hostomsky,
Karen Maegley,
David R. Newell,
Sheila Srinivasan, and
Bernard T. Golding
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4098-4108
3D-QSAR CoMFA on Cyclin-Dependent Kinase Inhibitors
Pierre Ducrot,
Michel Legraverend, and
David S. Grierson
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4109-4117
Active Site Binding Modes of HIV-1 Integrase Inhibitors
Christoph A. Sotriffer,
Haihong Ni, and
J. Andrew McCammon
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4118-4125
Conformationally Constrained Anesthetic Steroids That Modulate GABAA Receptors
Alison Anderson,
Andrew C. Boyd,
John K. Clark,
Lee Fielding,
David K. Gemmell,
Niall M. Hamilton,
Maurice S. Maidment,
Valerie May,
Ross McGuire,
Petula McPhail,
Francis H. Sansbury,
Hardy Sundaram, and
Robert Taylor
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4126-4134
Thio- and Oxoflavopiridols, Cyclin-Dependent Kinase 1-Selective Inhibitors: Synthesis and Biological Effects
Kyoung Soon Kim,
John S. Sack,
John S. Tokarski,
Ligang Qian,
Sam T. Chao,
Leslie Leith,
Yolanda F. Kelly,
Raj N. Misra,
John T. Hunt,
S. David Kimball,
William G. Humphreys,
Barris S. Wautlet,
Janet G. Mulheron, and
Kevin R. Webster
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4135-4150
Adenosine Analogues as Inhibitors of Trypanosoma brucei Phosphoglycerate Kinase: Elucidation of a Novel Binding Mode for a 2-Amino-N6-Substituted Adenosine
Jerome C. Bressi,
Jungwoo Choe,
Melinda T. Hough,
Frederick S. Buckner,
Wesley C. Van Voorhis,
Christophe L. M. J. Verlinde,
Wim G. J. Hol, and
Michael H. Gelb
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4151-4159
2D QSAR Modeling and Preliminary Database Searching for Dopamine Transporter Inhibitors Using Genetic Algorithm Variable Selection of Molconn Z Descriptors
Brian T. Hoffman,
Theresa Kopajtic,
Jonathan L. Katz, and
Amy Hauck Newman
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4160-4168
Sulfoxide-Containing Aromatic Nitrogen Mustards as Hypoxia-Directed Bioreductive Cytotoxins
Zhong-Yue Sun,
Emad Botros,
Ai-Duen Su,
Yu Kim,
Enju Wang,
Nesrine Z. Baturay, and
Chul-Hoon Kwon
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4169-4179
The Mitochondrial Monoamine Oxidase-Aldehyde Dehydrogenase Pathway: A Potential Site of Action of Daidzin
Nadège Rooke,
Dian-Jun Li,
Junqing Li, and
Wing Ming Keung
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4180-4188
Calculation and Prediction of Binding Free Energies for the Matrix Metalloproteinases
Oreola A. T. Donini and
Peter A. Kollman
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4189-4199
Synthesis and Biological Evaluation of Ceramide Analogues with Substituted Aromatic Rings or an Allylic Fluoride in the Sphingoid Moiety
Ilse Van Overmeire,
Swetlana A. Boldin,
Krishnan Venkataraman,
Rivka Zisling,
Steven De Jonghe,
Serge Van Calenbergh,
Denis De Keukeleire,
Anthony H. Futerman, and
Piet Herdewijn
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4200-4211
3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and Related 2-Urea Derivatives Are Potent and Selective Inhibitors of the FGF Receptor-1 Tyrosine Kinase
Andrew M. Thompson,
Cleo J. C. Connolly,
James M. Hamby,
Stacey Boushelle,
Brian G. Hartl,
Aneesa M. Amar,
Alan J. Kraker,
Denise L. Driscoll,
Randall W. Steinkampf,
Sandra J. Patmore,
Patrick W. Vincent,
Bill J. Roberts,
William L. Elliott,
Wayne Klohs,
Wilbur R. Leopold,
H. D. Hollis Showalter, and
William A. Denny
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4212-4218
Inhibition of Protein Synthesis by Didemnins: Cell Potency and SAR
Deepika Ahuja,
Adam Geiger,
Joshi M. Ramanjulu,
Matthew D. Vera,
Bhagyashri SirDeshpande,
Amy Pfizenmayer,
Mohamed Abazeed,
Daniel J. Krosky,
David Beidler,
Madeleine M. Joullié, and
Peter L. Toogood
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4219-4227
Novel Bronchodilators: Synthesis, Transamination Reactions, and Pharmacology of a Series of Pyrazino[2,3-c][1,2,6]thiadiazine 2,2-Dioxides
Nuria Campillo,
Concepción García,
Pilar Goya,
Ibon Alkorta, and
Juan A. Páez
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4228-4232
Syntheses and Antimalarial Activities of 10-Substituted Deoxoartemisinins
Jingyuan Ma,
Esther Katz,
Dennis E. Kyle, and
Herman Ziffer
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4233-4246
Synthetic Oleanane and Ursane Triterpenoids with Modified Rings A and C: A Series of Highly Active Inhibitors of Nitric Oxide Production in Mouse Macrophages
Tadashi Honda,
BarbieAnn V. Rounds,
Lothar Bore,
Heather J. Finlay,
Frank G. Favaloro, Jr.,
Nanjoo Suh,
Yongping Wang,
Michael B. Sporn, and
Gordon W. Gribble
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4247-4265
Synthesis, Biological Evaluation, and Conformational Analysis of A-Ring Diastereomers of 2-Methyl-1,25-dihydroxyvitamin D3 and Their 20-Epimers: Unique Activity Profiles Depending on the Stereochemistry of the A-Ring and at C-20
Katsuhiro Konno,
Toshie Fujishima,
Shojiro Maki,
Zhaopeng Liu,
Daishiro Miura,
Manabu Chokki,
Seiichi Ishizuka,
Kentaro Yamaguchi,
Yukiko Kan,
Masaaki Kurihara,
Naoki Miyata,
Connie Smith,
Hector F. DeLuca, and
Hiroaki Takayama
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4266-4277
Synthesis and Evaluation of Novel Steroidal Oxime Inhibitors of P450 17 (17-Hydroxylase/C17-20-Lyase) and 5-Reductase Types 1 and 2
Rolf W. Hartmann,
Markus Hector,
Samer Haidar,
Peter B. Ehmer,
Wolfgang Reichert, and
Joachim Jose
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4278-4287
Contribution of the Adenine Base to the Activity of Adenophostin A Investigated Using a Base Replacement Strategy
Rachel D. Marwood,
David J. Jenkins,
Vanessa Correa,
Colin W. Taylor, and
Barry V. L. Potter
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4288-4312
Structure-Activity Relationships of a Series of Pyrrolo[3,2-d]pyrimidine Derivatives and Related Compounds as Neuropeptide Y5 Receptor Antagonists
Mark H. Norman,
Ning Chen,
Zhidong Chen,
Christopher Fotsch,
Clarence Hale,
Nianhe Han,
Ray Hurt,
Tracy Jenkins,
John Kincaid,
Longbin Liu,
Yuelie Lu,
Ofir Moreno,
Vincent J. Santora,
Jennifer D. Sonnenberg, and
William Karbon
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4313-4318
Synthesis and Biological Activity of Novel 5-Fluoro-2'-deoxyuridine Phosphoramidate Prodrugs
Caren L. Freel Meyers,
Liping Hong,
Carolyn Joswig, and
Richard F. Borch
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4319-4327
Activation Mechanisms of Nucleoside Phosphoramidate Prodrugs
Caren L. Freel Meyers and
Richard F. Borch
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BRIEF ARTICLES
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4328-4331
Hydrolytic Stability versus Ring Size in Lactams: Implications for the Development of Lactam Antibiotics and Other Serine Protease Inhibitors
Peter Imming,
Bernhard Klar, and
Dorothea Dix
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BOOK REVIEWS
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4332-4332
Chromatography: Methods and Protocols. Volume 147, Methods in Molecular Biology Edited by Pascal Bailon, George K. Ehrlich, Wen-Jian Fung, and Wolfgang Berthold. Humana Press, Totowa, NJ. 2000. x + 230 pp. 15.5 × 23.5 cm. ISBN 0-89603-694-4. $79.50.
Greg T. Hermanson
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