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COMMUNICATIONS
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3421-3424
| A Multisubstrate Adduct Inhibitor of AICAR Transformylase
Mark Wall,
Jae Hoon Shim, and
Stephen J. Benkovic
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3425-3435
Conceptually New Sulfone Analogues of the Hormone 1 ,25-Dihydroxyvitamin D3: Synthesis and Preliminary Biological Evaluation
Gary H. Posner,
Qiang Wang,
Gyoonhee Han,
Jae Kyoo Lee,
Kenneth Crawford,
Sarvenaz Zand,
Henry Brem,
Sara Peleg,
Patrick Dolan, and
Thomas W. Kensler
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3436-3446
| Probing the Binding of Indolactam-V to Protein Kinase C through Site-Directed Mutagenesis and Computational Docking Simulations
Shaomeng Wang,
Ming Liu,
Nancy E. Lewin,
Patricia S. Lorenzo,
Dipak Bhattacharrya,
Lixin Qiao,
Alan P. Kozikowski, and
Peter M. Blumberg
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ARTICLES
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3447-3462
Synthesis of Novel GABA Uptake Inhibitors. 3. Diaryloxime and Diarylvinyl Ether Derivatives of Nipecotic Acid and Guvacine as Anticonvulsant Agents
Lars J. S. Knutsen,
Knud Erik Andersen,
Jesper Lau,
Behrend F. Lundt,
Rodger F. Henry,
Howard E. Morton,
Lars Nærum,
Hans Petersen,
Henrik Stephensen,
Peter D. Suzdak,
Michael D. B. Swedberg,
Christian Thomsen, and
Per O. S rensen
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3463-3477
| N-Substituted Adenosines as Novel Neuroprotective A1 Agonists with Diminished Hypotensive Effects
Lars J. S. Knutsen,
Jesper Lau,
Hans Petersen,
Christian Thomsen,
Jan U. Weis,
Michael Shalmi,
Martin E. Judge,
Anker Jon Hansen, and
Malcolm J. Sheardown
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3478-3485
| Synthesis of 1-(2-Aminophenyl)isoquinolines and the Biological Activity of Their cis-Dichloro Platinum(II) Complexes
Franz von Nussbaum,
Bernhard Miller,
Stefan Wild,
Christoph S. Hilger,
Susanne Schumann,
Haralabos Zorbas,
Wolfgang Beck, and
Wolfgang Steglich
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3486-3493
| Substituted Analogues of GV150526 as Potent Glycine Binding Site Antagonists in Animal Models of Cerebral Ischemia
Romano Di Fabio,
Nadia Conti,
Elisabetta De Magistris,
Aldo Feriani,
Stefano Provera,
Fabio Maria Sabbatini,
Angelo Reggiani,
Luca Rovatti, and
Robert J. Barnaby
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3494-3501
8,11-Dihydroxy-6-[(aminoalkyl)amino]-7H-benzo[e]perimidin-7-ones with Activity in Multidrug-Resistant Cell Lines: Synthesis and Antitumor Evaluation
Barbara Stefa ska,
Maria Dzieduszycka,
Maria M. Bontemps-Gracz, and
Edward Borowski
, Sante Martelli
, Rosanna Supino,
Graziella Pratesi,
MichelAndrea De Cesare, and
Franco Zunino
, Halina Ku nierczyk and
Czes aw Radzikowski
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3502-3509
| CoMFA Study of Novel Phenyl Ring-Substituted 3-(Diphenylmethoxy)tropane Analogues at the Dopamine Transporter
Amy Hauck Newman,
Sari Izenwasser,
Michael J. Robarge, and
Richard H. Kline
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3510-3519
| 5-Deazafolate Analogues with a Rotationally Restricted Glutamate or Ornithine Side Chain: Synthesis and Binding Interaction with Folylpolyglutamate Synthetase
Andre Rosowsky,
Ronald A. Forsch,
Allison Null, and
Richard G. Moran
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3520-3526
The Opioid  Agonist/ Antagonist DIPP-NH2[ ] Produces a Potent Analgesic Effect, No Physical Dependence, and Less Tolerance than Morphine in Rats
Peter W. Schiller,
Marian E. Fundytus,
Lisa Merovitz,
Grazyna Weltrowska,
Thi M.-D. Nguyen,
Carole Lemieux,
Nga N. Chung, and
Terence J. Coderre
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3527-3538
| Synthesis, Opioid Receptor Binding, and Biological Activities of Naltrexone-Derived Pyrido- and Pyrimidomorphinans
Subramaniam Ananthan,
Hollis S. Kezar III,
Ronald L. Carter,
Surendra K. Saini,
Kenner C. Rice,
Jennifer L. Wells,
Peg Davis,
Heng Xu,
Christina M. Dersch,
Edward J. Bilsky,
Frank Porreca, and
Richard B. Rothman
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3539-3556
| Synthesis, Biological Activity, and Conformational Analysis of Four seco-D-15,19-bisnor-1,25-Dihydroxyvitamin D Analogues, Diastereomeric at C17 and C20
Xiaoming Zhou,
Gui-Dong Zhu,
Dirk Van Haver,
Maurits Vandewalle,
Pierre J. De Clercq,
Annemieke Verstuyf, and
Roger Bouillon
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3557-3571
| Design and Structure-Activity Relationships of Potent and Selective Inhibitors of Blood Coagulation Factor Xa
William R. Ewing,
Michael R. Becker,
Vincent E. Manetta,
Roderick S. Davis,
Henry W. Pauls,
Helen Mason,
Yong Mi Choi-Sledeski,
Daniel Green,
Don Cha,
Alfred P. Spada,
Daniel L. Cheney,
Jonathan S. Mason,
Sebastien Maignan,
Jean-Pierre Guilloteau,
Karen Brown,
Dennis Colussi,
Ross Bentley,
Jeff Bostwick,
Charles J. Kasiewski,
Suzanne R. Morgan,
Robert J. Leadley,
Christopher T. Dunwiddie,
Mark H. Perrone, and
Valeria Chu
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3572-3587
| Sulfonamidopyrrolidinone Factor Xa Inhibitors: Potency and Selectivity Enhancements via P-1 and P-4 Optimization
Yong Mi Choi-Sledeski,
Daniel G. McGarry,
Daniel M. Green,
Helen J. Mason,
Michael R. Becker,
Roderick S. Davis,
William R. Ewing,
William P. Dankulich,
Vincent E. Manetta,
Robert L. Morris,
Alfred P. Spada,
Daniel L. Cheney,
Karen D. Brown,
Dennis J. Colussi,
Valeria Chu,
Christopher L. Heran,
Suzanne R. Morgan,
Ross G. Bentley,
Robert J. Leadley,
Sebastien Maignan,
Jean-Pierre Guilloteau,
Christopher T. Dunwiddie, and
Henry W. Pauls
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3588-3601
| Synthesis and Biochemical Evaluation of 3-Fluoromethyl-1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the 2-Adrenoceptor
Gary L. Grunewald,
Timothy M. Caldwell,
Qifang Li,
Meri Slavica,
Kevin R. Criscione,
Ronald T. Borchardt, and
Wen Wang
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3602-3614
Synthesis, Structure-Activity Relationships, and RAR -Ligand Interactions of Nitrogen Heteroarotinoids
Arindam Dhar,
Shengquan Liu,
Jozef Klucik,
K. Darrell Berlin,
Matora M. Madler,
Shennan Lu,
R. Todd Ivey,
David Zacheis,
Chad W. Brown,
E. C. Nelson,
Paul J. Birckbichler, and
Doris M. Benbrook
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3615-3622
| Synthesis and Cytotoxic Evaluation of Cycloheximide Derivatives as Potential Inhibitors of FKBP12 with Neuroregenerative Properties
Claudia Christner,
Ralf Wyrwa,
Silvia Marsch,
Gerhard Küllertz,
Ralf Thiericke,
Susanne Grabley,
Dieter Schumann, and
Gunter Fischer
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3623-3628
| Design and Synthesis of Water-Soluble Glucuronide Derivatives of Camptothecin for Cancer Prodrug Monotherapy and Antibody-Directed Enzyme Prodrug Therapy (ADEPT)
Yu-Ling Leu,
Steve R. Roffler, and
Ji-Wang Chern
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3629-3635
| Allosteric Modulation of the Adenosine A1 Receptor. Synthesis and Biological Evaluation of Novel 2-Amino-3-benzoylthiophenes as Allosteric Enhancers of Agonist Binding
Pieter A. M. van der Klein,
Angeliki P. Kourounakis, and
Ad P. IJzerman
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3636-3646
| 2-Thioether 5'-O-(1-Thiotriphosphate)adenosine Derivatives as New Insulin Secretagogues Acting through P2Y-Receptors
Bilha Fischer,
Ana Chulkin,
Jose L. Boyer,
Kendall T. Harden,
Fernand-Pierre Gendron,
Adrien R. Beaudoin,
Jeannie Chapal,
Dominique Hillaire-Buys, and
Pierre Petit
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3647-3656
| Design, Synthesis, and Biological Evaluation of Novel Non-Piperazine Analogues of 1-[2-(Diphenylmethoxy)ethyl]- and 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines as Dopamine Transporter Inhibitors
Sung-Woon Choi,
David R. Elmaleh,
Robert N. Hanson, and
Alan J. Fischman
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3657-3667
| Drug Delivery Systems Employing 1,4- or 1,6-Elimination: Poly(ethylene glycol) Prodrugs of Amine-Containing Compounds
Richard B. Greenwald,
Annapurna Pendri,
Charles D. Conover,
Hong Zhao,
Yun H. Choe,
Anthony Martinez,
Kwok Shum, and
Shuiyun Guan
[Full Article - PDF]
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3668-3678
| Pyrrolidine-3-carboxylic Acids as Endothelin Antagonists. 4. Side Chain Conformational Restriction Leads to ETB Selectivity
Thomas W. von Geldern,
Andrew S. Tasker,
Bryan K. Sorensen,
Martin Winn,
Bruce G. Szczepankiewicz,
Douglas B. Dixon,
William J. Chiou,
Liming Wang,
Jerry L. Wessale,
Andy Adler,
Kennan C. Marsh,
Bach Nguyen, and
Terry J. Opgenorth
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3679-3689
| Design, Synthesis, and Activity of a Series of Pyrrolidine-3-carboxylic Acid-Based, Highly Specific, Orally Active ETB Antagonists Containing a Diphenylmethylamine Acetamide Side Chain
Gang Liu,
Natasha S. Kozmina,
Martin Winn,
Thomas W. von Geldern,
William J. Chiou,
Douglas B. Dixon,
Bach Nguyen,
Kennan C. Marsh, and
Terry J. Opgenorth
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3690-3700
| Carbonic Anhydrase Inhibitors: Synthesis of Water-Soluble, Aminoacyl/Dipeptidyl Sulfonamides Possessing Long-Lasting Intraocular Pressure-Lowering Properties via the Topical Route
Andrea Scozzafava,
Fabrizio Briganti,
Giovanna Mincione,
Luca Menabuoni,
Francesco Mincione, and
Claudiu T. Supuran
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3701-3710
| Second-Generation Peptidomimetic Inhibitors of Protein Farnesyltransferase Demonstrating Improved Cellular Potency and Significant in Vivo Efficacy
Stephen J. O'Connor,
Kenneth J. Barr,
Le Wang,
Bryan K. Sorensen,
Andrew S. Tasker,
Hing Sham,
Shi-Chung Ng,
Jerome Cohen,
Edward Devine,
Sajeev Cherian,
Badr Saeed,
Haichao Zhang,
Jang Yun Lee,
Robert Warner,
Stephen Tahir,
Peter Kovar,
Patricia Ewing,
Jeffrey Alder,
Michael Mitten,
Juan Leal,
Kennan Marsh,
Joy Bauch,
Daniel J. Hoffman,
Said M. Sebti, and
Saul H. Rosenberg
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3711-3717
| Cardioselective Antiischemic ATP-Sensitive Potassium Channel (KATP) Openers. 6. Effect of Modifications at C6 of Benzopyranyl Cyanoguanidines
Charles Z. Ding,
George C. Rovnyak,
Raj N. Misra,
Gary J. Grover,
Arthur V. Miller,
Syed Z. Ahmed,
Yolanda Kelly,
Diane E. Normandin,
Paul G. Sleph, and
Karnail S. Atwal
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3718-3725
| Design, Synthesis, and Evaluation of Chromen-2-ones as Potent and Selective Human Dopamine D4 Antagonists
Suzanne R. Kesten,
Thomas G. Heffner,
Stephen J. Johnson,
Thomas A. Pugsley,
Jonathan L. Wright, and
Lawrence D. Wise
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3726-3731
| Lobeline: Structure-Affinity Investigation of Nicotinic Acetylcholinergic Receptor Binding
Dwight Flammia,
Malgorzata Dukat,
M. Imad Damaj,
Billy Martin, and
Richard A. Glennon
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3732-3736
| IFN--Derived Lipopeptides: Influence of Lipid Modification on the Conformation and the Ability To Induce MHC Class II Expression on Murine and Human Cells
Kader Thiam,
Estelle Loing,
Claudie Verwaerde,
Claude Auriault, and
Hélène Gras-Masse
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3737-3741
| Small Peptides Containing Phosphotyrosine and Adjacent Me-Phosphotyrosine or Its Mimetics as Highly Potent Inhibitors of Grb2 SH2 Domain
Wang-Qing Liu,
Michel Vidal,
Nohad Gresh,
Bernard P. Roques, and
Christiane Garbay
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3742-3742
| Peptidomimetic Protocols Edited by Wieslaw M. Kazmierski. Humana Press, Totowa, NJ. 1999. xxx + 549 pp. 15.5 × 24 cm. ISBN 0-846-03517-4. $89.50.
D. Eric Walters
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