PERSPECTIVES
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3453-3473
Platelet Glycoprotein IIb-IIIa Antagonists as Prototypical Integrin Blockers: Novel Parenteral and Potential Oral Antithrombotic Agents
Robert M. Scarborough and
Daniel D. Gretler
[Full Article -
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3474-3477
(S)-4-Methyl-2-(methylamino)pentanoic Acid [4,4-Bis(4-fluorophenyl)butyl]amide Hydrochloride, a Novel Calcium Channel Antagonist, Is Efficacious in Several Animal Models of Pain
Yuntao Song,
S. Scott Bowersox,
David T. Connor,
David J. Dooley,
Susan M. Lotarski,
Thomas Malone,
George Miljanich,
Elizabeth Millerman,
Michael F. Rafferty,
David Rock,
Bruce D. Roth,
Joann Schmidt,
Sally Stoehr,
Balazs G. Szoke,
Charles Taylor,
Mark Vartanian, and
Yong-Xiang Wang
[Full Article -
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3478-3481
Bis-Quinolinium Cyclophanes: 8,14-Diaza-1,7(1,4)-diquinolinacyclotetradecaphane (UCL 1848), a Highly Potent and Selective, Nonpeptidic Blocker of the Apamin-Sensitive Ca2+-Activated K+ Channel
Jian-Qing Chen,
Dimitrios Galanakis,
C. Robin Ganellin,
Philip M. Dunn, and
Donald H. Jenkinson
[Full Article -
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3482-3486
BCX-1812 (RWJ-270201): Discovery of a Novel, Highly Potent, Orally Active, and Selective Influenza Neuraminidase Inhibitor through Structure-Based Drug Design
Y. Sudhakar Babu,
Pooran Chand,
Shanta Bantia,
Pravin Kotian,
Ali Dehghani,
Yahya El-Kattan,
Tsu-Hsing Lin,
Tracy L. Hutchison,
Arthur J. Elliott,
Cynthia D. Parker,
Sandya L. Ananth,
LaShun L. Horn,
Graeme W. Laver, and
John A. Montgomery
[Full Article -
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EXPEDITED ARTICLES
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3487-3494
Discovery of a Potent, Highly Selective, and Orally Efficacious Small-Molecule Activator of the Insulin Receptor
Kun Liu,
Libo Xu,
Deborah Szalkowski,
Zhihua Li,
Victor Ding,
Gloria Kwei,
Su Huskey,
David E. Moller,
James V. Heck,
Bei B. Zhang, and
A. Brian Jones[Full Article -
PDF]
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ARTICLES
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3495-3504
Synthesis, Stability, Antiviral Activity, and Protease-Bound Structures of Substrate-Mimicking Constrained Macrocyclic Inhibitors of HIV-1 Protease
Joel D. A. Tyndall,
Robert C. Reid,
David P. Tyssen,
Darren K. Jardine,
Belinda Todd,
Margaret Passmore,
Darren R. March,
Leonard K. Pattenden,
Douglas A. Bergman,
Dianne Alewood,
Shu-Hong Hu,
Paul F. Alewood,
Christopher J. Birch,
Jennifer L. Martin, and
David P. Fairlie[Full Article -
PDF]
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3505-3517
Development of Peptide 3D Structure Mimetics: Rational Design of Novel Peptoid Cholecystokinin Receptor Antagonists
Caroline M. R. Low,
James W. Black,
Howard B. Broughton,
Ildiko M. Buck,
Jonathan M. R. Davies,
David J. Dunstone,
Robert A. D. Hull,
S. Barret Kalindjian,
Iain M. McDonald,
Michael J. Pether,
Nigel P. Shankley, and
Katherine I. M. Steel[Full Article -
PDF]
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3518-3529
2,7-Dioxo-2,3,4,5,6,7-hexahydro-1H-benzo[h][1,4]diazonine as a New Template for the Design of CCK2 Receptor Antagonists
Iain M. McDonald,
David J. Dunstone,
S. Barret Kalindjian,
Ian D. Linney,
Caroline M. R. Low,
Michael J. Pether,
Katherine I. M. Steel,
Matthew J. Tozer, and
J. G. Vinter[Full Article -
PDF]
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3530-3540
Design and Solution Structure of Functional Peptide Mimetics of Nerve Growth Factor
Natalia Beglova,
Sergei Maliartchouk,
Irena Ekiel,
Maria Clara Zaccaro,
H. Uri Saragovi, and
Kalle Gehring[Full Article -
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3541-3548
Gold(III) Complexes as Potential Antitumor Agents: Solution Chemistry and Cytotoxic Properties of Some Selected Gold(III) Compounds
Luigi Messori,
Francesco Abbate,
Giordana Marcon,
Pierluigi Orioli,
Marco Fontani,
Enrico Mini,
Teresita Mazzei,
Stefania Carotti,
Tim O'Connell, and
Piero Zanello[Full Article -
PDF]
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3549-3557
Thiazoloindans and Thiazolobenzopyrans: A Novel Class of Orally Active Central Dopamine (Partial) Agonists
L. Alexander van Vliet,
Nienke Rodenhuis, and
Håkan Wikström
, Thomas A. Pugsley,
Kevin A. Serpa,
Leonard T. Meltzer,
Thomas G. Heffner, and
Lawrence D. Wise
, Mary E. Lajiness,
Rita M. Huff, and
Kjell Svensson
, Guido R. M. M. Haenen and
Aalt Bast[Full Article -
PDF]
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3558-3565
Selective Protection and Functionalization of Morphine: Synthesis and Opioid Receptor Binding Properties of 3-Amino-3-desoxymorphine Derivatives,1
Mark P. Wentland,
Wenhu Duan,
Dana J. Cohen, and
Jean M. Bidlack[Full Article -
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3566-3572
Bis(2-(Acylamino)phenyl) Disulfides, 2-(Acylamino)benzenethiols, and S-(2-(Acylamino)phenyl) Alkanethioates as Novel Inhibitors of Cholesteryl Ester Transfer Protein
Hisashi Shinkai,
Kimiya Maeda,
Takahiro Yamasaki,
Hiroshi Okamoto, and
Itsuo Uchida[Full Article -
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BRIEF ARTICLES
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3573-3576
Studies Directed at the Use of a Parallel Synthesis Matrix to Increase Throughput in an in Vivo Assay
Andrea Leone-Bay,
John Freeman,
Doris O'Toole,
Connie Rosado-Gray,
Sirpa Salo-Kostmayer,
Monica Tai,
Frank Mercogliano, and
Robert A. Baughman[Full Article -
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3577-3580
Preparation and Biological Activity of Amino Acid and Peptide Conjugates of Antitumor Hydroxymethylacylfulvene
Trevor C. McMorris,
Jian Yu,
Huan-Tony Ngo,
Haixia Wang, and
Michael J. Kelner[Full Article -
PDF]
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3581-3586
Conceptually New 20-epi-22-Oxa Sulfone Analogues of the Hormone 1,25-Dihydroxyvitamin D3: Synthesis and Biological Evaluation
Gary H. Posner,
Kenneth Crawford,
Mei-Ling Siu-Caldera,
G. Satyanarayana Reddy,
Stephen F. Sarabia,
David Feldman,
Evelyne van Etten,
Chantal Mathieu,
Lynn Gennaro,
Paul Vouros,
Sara Peleg,
Patrick M. Dolan, and
Thomas W. Kensler[Full Article -
PDF]
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