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

Autor:	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
Jazyk:	angličtina
Rok vydání:	2012
Předmět:	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
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ace88350b0677b6d5e549d1aab456577 https://europepmc.org/articles/PMC4025772/ Zobrazit plný text záznamu