Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potent β isoform selective phosphatidylinositol 3-kinase inhibitors.
| Autor: | Sanchez RM; Cancer Metabolism Chemistry, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA. robert.m.sanchez@gsk.com, Erhard K, Hardwicke MA, Lin H, McSurdy-Freed J, Plant R, Raha K, Rominger CM, Schaber MD, Spengler MD, Moore ML, Yu H, Luengo JI, Tedesco R, Rivero RA |
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| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 May 01; Vol. 22 (9), pp. 3198-202. Date of Electronic Publication: 2012 Mar 16. |
| DOI: | 10.1016/j.bmcl.2012.03.039 |
| Abstrakt: | A series of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones with excellent enzyme inhibition, improved isoform selectivity, and excellent inhibition of downstream phosphorylation of AKT has been identified. Several compounds in the series demonstrated potent (∼ 0.100 μM IC(50)) growth inhibition in a PTEN deficient cancer cell line. (Copyright © 2012 Elsevier Ltd. All rights reserved.) |
| Databáze: | MEDLINE |
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