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Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase

✍ Scribed by Steven T. Staben; Timothy P. Heffron; Daniel P. Sutherlin; Seema R. Bhat; Georgette M. Castanedo; Irina S. Chuckowree; Jenna Dotson; Adrian J. Folkes; Lori S. Friedman; Leslie Lee; John Lesnick; Cristina Lewis; Jeremy M. Murray; Jim Nonomiya; Alan G. Olivero; Emile Plise; Jodie Pang; Wei Wei Prior; Laurent Salphati; Lionel Rouge; Deepak Sampath; Vickie Tsui; Nan Chi Wan; Shumei Wang; Christian Weismann; Ping Wu; Bing-Yan Zhu

Book ID: 104004791
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 1007 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.08.067

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✦ Synopsis

a b s t r a c t

Starting from HTS hit 1a, X-ray co-crystallization and molecular modeling were used to design potent and selective inhibitors of PI3-kinase. Bioavailablity in this series was improved through careful modulation of physicochemical properties. Compound 12 displayed in vivo knockdown of PI3K pharmacodynamic markers such as pAKT, pPRAS40, and pS6RP in a PC3 prostate cancer xenograft model.

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