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Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors

作者	LIN HONG; SCHULZ MARK J; XIE REN; ZENG JIN; LUENGO JUAN I; SQUIRE MICHAEL D; TEDESCO ROSANNA; QU JUNYA; ERHARD KARL; MACK JAMES F; RAHA KAUSHIK; PLANT RAMONA; ROMINGER CYNTHIA M; ARIAZI JENNIFER L; SHERK CHRISTIAN S; SCHABER MICHAEL D; MCSURDYFREED JEANELLE; SPENGLER MICHAEL D; DAVIS CHARLES B; HARDWICKE MARY ANN; RIVERO RALPH A

选自	期刊 ACS Medicinal Chemistry Letters; 卷期 2012年3-7; 页码 524-529

关联知识点

[摘要]：A novel thiazolopyrimidinone series of PI3K-beta selective inhibitors has been identified. This chemotype has provided an excellent tool compound, 18, that showed potent growth inhibition in the PTEN-deficient breast cancer cell line MDA-MB-468 Under anchorage independent conditions, and it also demonstrated pharmacodynamic effects and efficacy in a PTEN-deficient prostate cancer PC-3 xenograft mouse model.
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