Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors
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- 作者：Hong Lin ; Mark J. Schulz ; Ren Xie ; Jin Zeng ; Juan I. Luengo ; Michael D. Squire ; Rosanna Tedesco ; Junya Qu ; Karl Erhard ; James F. Mack ; Kaushik Raha ; Ramona Plant ; Cynthia M. Rominger ; Jennifer L. Ariazi ; Christian S. Sherk ; Michael D. Schaber ; Jeanelle McSurdy-Freed ; Michael D. Spengler ; Charles B. Davis ; Mary Ann Hardwicke ; Ralph A. Rivero
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2012
- 出版时间：July 12, 2012
- 年：2012
- 卷：3
- 期：7
- 页码：524-529
- 全文大小：354K
- 年卷期：v.3,no.7(July 12, 2012)
- ISSN：1948-5875
文摘
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.