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

Charles B. Davis (688677); Christian S. Sherk (2065378); Cynthia M. Rominger (1450621); Hong Lin (46089); James F. Mack (2018785); Jeanelle McSurdy-Freed (1993057); Jennifer
L. Ariazi (2065381); Jin Zeng (196246); Juan I. Luengo (1450612); Junya Qu (1450561); Karl Erhard (1993066); Kaushik Raha (1370313); Mark J. Schulz (1450624); Mary Ann Hardwicke (1450582); Michael
D. Squire (2065387); Michael D. Schaber (1370355); Michael D. Spengler (2065384); Ralph
A. Rivero (2065375); Ramona Plant (1993051); Ren Xie (1450564); Rosanna Tedesco (1450573)

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

Abstract

A novel thiazolopyrimidinone series of PI3K-beta selective inhibitors has been identified. This chemotype has provided an excellent tool compound, <b>18</b>, 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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Last time updated on 16/03/2018