| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10592500 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
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 (⼠0.100 μM IC50) growth inhibition in a PTEN deficient cancer cell line.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
![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](/preview/png/10592500.png "First Page Preview: 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")
Authors
Robert M. Sanchez, Karl Erhard, Mary Ann Hardwicke, Hong Lin, Jeanelle McSurdy-Freed, Ramona Plant, Kaushik Raha, Cynthia M. Rominger, Michael D. Schaber, Michael D. Spengler, Michael L. Moore, Hongyi Yu, Juan I. Luengo, Rosanna Tedesco, Ralph A. Rivero,