- Zwitterionic CRTh2 Antagonists
[作者:LUKER TIM; BONNERT ROGER; PAINE STUART W; SCHMIDT JERZY; SARGENT CAROL; COOK ANTHONY R; COOK ANDREW; GARDINER PHILIP; HILL STEVE; WEYMANJONES CAROL; PATEL ANIL; THOM STEPHEN; THORNE PHILIP,期刊:Journal of Medicinal Chemistry, 页码:1779-1788 , 文章类型: Article,,卷期:2011年54-6]
- A novel series of zwitterions is reported that contains potent, selective antagonists of the chemoattractant receptor-homologous expressed on Th2 lymphocytes receptor (CRTh2 or DP2). A high quality lead compound 2 was di...
- Magnesium Chelating 2-Hydroxyisoquinoline-1,3(2H,4H)-diones, as Inhibitors of HIV-1 Integrase and/or the HIV-1 Reverse Transcriptase Ribonuclease H Domain: Discovery of a Novel Selective Inhibitor of the Ribonuclease H Function
[作者:BILLAMBOZ MURIEL; BAILLY FABRICE; LION CEDRIC; TOUATI NADIA; VEZIN HERVE; CALMELS CHRISTINA; ANDREOLA MARIELINE; CHRIST FRAUKE; DEBYSER ZEGER; COTELLE PHILIPPE,期刊:Journal of Medicinal Chemistry, 页码:1812-1824 , 文章类型: Article,,卷期:2011年54-6]
- 2-Hydroxyisoquinoline-1,3(2H,4H)-dione was recently discovered as a scaffold for the inhibition of HIV-1 integrase and the ribonuclease H function of HIV-1 reverse transcriptase. First, we investigate its interaction wit...
- Design and Optimization of Potent and Orally Bioavailable Tetrahydronaphthalene Raf Inhibitors
[作者:GOULD ALEXANDRA E; ADAMS RUTH; ADHIKARI SHARMILA; AERTGEERTS KATHLEEN; AFROZE ROUSHAN; BLACKBURN CHRISTOPHER; CALDERWOOD EMILY F; CHAU RYAN; CHOUITAR JOUHARA; DUFFEY MATTHEW O; ENGLAND DYLAN B; FARRER CHERYL; FORSYTH NANCY; GARCIA KHRISTOFER; GAULIN JEFFERY; GREENSPAN PAUL D; GUO RIBO; HARRISON SEAN J; HUAN SHIHCHUNG; IARTCHOUK NATALIA; JANOWICK DAVE; KIM MISOOK; KULKARNI BHEEMASHANKAR; LANGSTON STEVEN P; LIU JANE X; MA LITING; MENON SAURABH; MIZUTANI HIROTAKE; PASKE ERIN; RENOU CHRISTELLE C; REZAEI MANSOUREH; ROWLAND R SCOTT; SINTCHAK MICHAEL D; SMITH MICHAEL D; STROUD STEPHEN G; TREGAY MING; TIAN YUAN; VEIBY OLE P; VOS TRICIA J; VYSKOCIL STEPAN; WILLIAMS JULIET; XU TIANLIN; YANG JOHNNY J; YANO JASON; ZENG HONGBO; ZHANG DONG MEI; ZHANG QIN; GALVIN KATHERINE M,期刊:Journal of Medicinal Chemistry, 页码:1836-1846 , 文章类型: Article,,卷期:2011年54-6]
- Inhibition of mutant B-Raf signaling, through either direct inhibition of the enzyme or inhibition of MEK, the direct substrate of Raf, has been demonstrated preclinically to inhibit tumor growth. Very recently, treatmen...
- Structure-Based Design of Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 (PDK1) Inhibitors
[作者:MEDINA JESUS R; BECKER CHRISTOPHER J; BLACKLEDGE CHARLES W; DUQUENNE CELINE; FENG YANHONG; GRANT SETH W; HEERDING DIRK; LI WILLIAM H; MILLER WILLIAM H; ROMERIL STUART P; SCHERZER DARYL; SHU ARTHUR; BOBKO MARK A; CHADDERTON ANTONY R; DUMBLE MELISSA; GARDINER CHRISTINE M; GILBERT SETH; LIU QI; RABINDRAN SRIDHAR K; SUDAKIN VALERY; XIANG HONG; BRADY PAT G; CAMPOBASSO NINO; WARD PARIS; AXTEN JEFFREY M,期刊:Journal of Medicinal Chemistry, 页码:1871-1895 , 文章类型: Article,,卷期:2011年54-6]
- Phosphoinositide-dependent protein kinase-1 (PDK1) is a master regulator of the AGC family of kinases and an integral component of the PI3K/AKT/mTOR pathway. As this pathway is among the most commonly deregulated across ...
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