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- W2051091008 abstract "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." @default.
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- W2051091008 date "2010-10-01" @default.
- W2051091008 modified "2023-10-17" @default.
- W2051091008 title "Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase" @default.
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- W2051091008 doi "https://doi.org/10.1016/j.bmcl.2010.08.067" @default.
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