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

Authors :: Hong Lin
Charles B. Davis
Kaushik Raha
Ralph A. Rivero
Michael D. Schaber
Jeanelle McSurdy-Freed
Mary Ann Hardwicke
Karl F. Erhard
James F. Mack
Ren Xie
Michael D. Spengler
Ramona Plant
Cynthia M. Rominger
Junya Qu
Rosanna Tedesco
Jennifer L. Ariazi
Juan I. Luengo
Mark J. Schulz
Michael D. Squire
Christian S. Sherk
Jin Zeng
Publication Year :: 2012
Publisher :: American Chemical Society, 2012.
Abstract: 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.

Subjects :: business.industry
Organic Chemistry
Rational design
medicine.disease
Bioinformatics
Biochemistry
Prostate cancer
chemistry.chemical_compound
chemistry
Breast cancer cell line
Drug Discovery
Cancer research
Medicine
Structure–activity relationship
Homology modeling
Growth inhibition
business
Beta (finance)
PI3K/AKT/mTOR pathway

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