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4309-4312
Conformationally Constrained Analogues of Diacylglycerol. 18. The Incorporation of a Hydroxamate Moiety into Diacylglycerol-Lactones Reduces Lipophilicity and Helps Discriminate between sn-1 and sn-2 Binding Modes to Protein Kinase C (PK-C). Implications for Isozyme Specificity
Jeewoo Lee,
Kee-Chung Han,
Ji-Hye Kang,
Larry L. Pearce,
Nancy E. Lewin,
Shunqi Yan,
Samira Benzaria,
Marc C. Nicklaus,
Peter M. Blumberg, and
Victor E. Marquez
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4313-4324
Discovery of Small-Molecule Inhibitors of Bcl-2 through Structure-Based Computer Screening
Istvan J. Enyedy,
Yan Ling,
Kassoum Nacro,
York Tomita,
Xihan Wu,
Yeyu Cao,
Ribo Guo,
Bihua Li,
Xiaofeng Zhu,
Ying Huang,
Ya-Qiu Long,
Peter P. Roller,
Dajun Yang, and
Shaomeng Wang
[Full Article -
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4325-4338
Free Energy Component Analysis for Drug Design: A Case Study of HIV-1 Protease-Inhibitor Binding
Parul Kalra,
T. Vasisht Reddy, and
B. Jayaram
[Full Article -
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4339-4358
Oxindole-Based Inhibitors of Cyclin-Dependent Kinase 2 (CDK2): Design, Synthesis, Enzymatic Activities, and X-ray Crystallographic Analysis
H. Neal Bramson,
John Corona,
Stephen T. Davis,
Scott H. Dickerson,
Mark Edelstein,
Stephen V. Frye,
Robert T. Gampe, Jr.,
Phil A. Harris,
Anne Hassell,
William D. Holmes,
Robert N. Hunter,
Karen E. Lackey,
Brett Lovejoy,
Michael J. Luzzio,
Val Montana,
Warren J. Rocque,
David Rusnak,
Lisa Shewchuk,
James M. Veal,
Duncan H. Walker, and
Lee F. Kuyper
[Full Article -
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4359-4369
[1,2,4]Triazino[4,3-a]benzimidazole Acetic Acid Derivatives: A New Class of Selective Aldose Reductase Inhibitors
Federico Da Settimo,
Giampaolo Primofiore,
Antonio Da Settimo,
Concettina La Motta,
Sabrina Taliani,
Francesca Simorini,
Ettore Novellino,
Giovanni Greco,
Antonio Lavecchia, and
Enrico Boldrini
[Full Article -
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4370-4378
Cheminformatic Models To Predict Binding Affinities to Human Serum Albumin
Gonzalo Colmenarejo,
Ana Alvarez-Pedraglio, and
José-Luis Lavandera
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4379-4392
Systematic Structure-Based Design and Stereoselective Synthesis of Novel Multisubstituted Cyclopentane Derivatives with Potent Antiinfluenza Activity
Pooran Chand,
Pravin L. Kotian,
Ali Dehghani,
Yahya El-Kattan,
Tsu-Hsing Lin,
Tracy L. Hutchison,
Y. Sudhakar Babu,
Shanta Bantia,
Arthur J. Elliott, and
John A. Montgomery
[Full Article -
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4393-4403
Discovery of Novel p-Arylthio Cinnamides as Antagonists of Leukocyte Function-Associated Antigen-1/Intercellular Adhesion Molecule-1 Interaction. 4. Structure-Activity Relationship of Substituents on the Benzene Ring of the Cinnamide
Martin Winn,
Edward B. Reilly,
Gang Liu,
Jeffrey R. Huth,
Hwan-Soo Jae,
Jennifer Freeman,
Zhonghua Pei,
Zhili Xin,
John Lynch,
Jeff Kester,
Thomas W. von Geldern,
Sandra Leitza,
Peter DeVries,
Robert Dickinson,
Donna Mussatto, and
Gregory F. Okasinski
[Full Article -
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4404-4415
Synthesis and Structure-Activity Relationships of N-(1-Benzylpiperidin-4-yl)arylacetamide Analogues as Potent 1 Receptor Ligands
Yunsheng Huang,
Philip S. Hammond,
Li Wu, and
Robert H. Mach
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4416-4430
New Antimitotic Agents with Activity in Multi-Drug-Resistant Cell Lines and in Vivo Efficacy in Murine Tumor Models
Bruce G. Szczepankiewicz,
Gang Liu,
Hwan-Soo Jae,
Andrew S. Tasker,
Indrani W.Gunawardana,
Thomas W. von Geldern,
Stephen L. Gwaltney, II,
J. Ruth Wu-Wong,
Laura Gehrke,
William J. Chiou,
R. Bruce Credo,
Jeffery D. Alder,
Michael A. Nukkala,
Nicolette A. Zielinski,
Ken Jarvis,
Karl W. Mollison,
David J. Frost,
Joy L. Bauch,
Yu Hua Hui,
Akiyo K. Claiborne,
Qun Li, and
Saul H. Rosenberg
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4431-4442
trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: A New Class of Potent and Selective 5-HT1A Receptor Ligands as Conformationally Constrained Analogues of 4-[3-(5-Methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1- arylpiperazines
Roberto Perrone,
Francesco Berardi,
Nicola A. Colabufo,
Marcello Leopoldo,
Enza Lacivita, and
Vincenzo Tortorella
, Amedeo Leonardi,
Elena Poggesi, and
Rodolfo Testa
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4443-4452
Antimalarial Alkoxylated and Hydroxylated Chalones: Structure-Activity Relationship Analysis
Mei Liu,
Prapon Wilairat, and
Mei-Lin Go
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4453-4461
Novel Tropane-Based Irreversible Ligands for the Dopamine Transporter
Mu-Fa Zou,
Theresa Kopajtic,
Jonathan L. Katz,
Sara Wirtz,
Joseph B. Justice, Jr., and
Amy Hauck Newman
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4462-4467
O-Phosphonatomethylcholine, Its Analogues, Alkyl Esters, and Their Biological Activity
Antonín Hol,
Berta Otová,
Milo Budínsk,
David Emerson, and
Marc E. Wiles
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4468-4474
3-(Arylacetylamino)-N-methylbenzamides: A Novel Class of Selective Anti-Helicobacter pylori Agents
Ryoichi Ando,
Makoto Kawamura, and
Noriko Chiba
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4475-4480
Synthesis and Biological Studies of Novel Nucleoside Phosphoramidate Prodrugs
Sandra C. Tobias and
Richard F. Borch
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4481-4491
Nonsteroidal Selective Glucocorticoid Modulators: the Effect of C-5 Alkyl Substitution on the Transcriptional Activation/Repression Profile of 2,5-Dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines
Steven W. Elmore,
Michael J. Coghlan,
David D. Anderson,
John K. Pratt,
Brian E. Green,
Alan X. Wang,
Michael A. Stashko,
Chun W. Lin,
Curtis M. Tyree,
Jeffery N. Miner,
Peer B. Jacobson,
Denise M. Wilcox, and
Benjamin C. Lane
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4492-4496
Design, Synthesis, and Biological Activity of a Novel Non-Cisplatin-type Platinum-Acridine Pharmacophore
Elizabeth T. Martins,
Hemanta Baruah,
Jaroslaw Kramarczyk,
Gilda Saluta,
Cynthia S. Day,
Gregory L. Kucera, and
Ulrich Bierbach
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