1366126-75-1Relevant academic research and scientific papers
Synthesis and structure-activity relationships of imidazo[1,2-a]pyrimidin- 5(1H)-ones as a novel series of beta isoform selective phosphatidylinositol 3-kinase inhibitors
Lin, Hong,Erhard, Karl,Hardwicke, Mary Ann,Luengo, Juan I.,MacK, James F.,McSurdy-Freed, Jeanelle,Plant, Ramona,Raha, Kaushik,Rominger, Cynthia M.,Sanchez, Robert M.,Schaber, Michael D.,Schulz, Mark J.,Spengler, Michael D.,Tedesco, Rosanna,Xie, Ren,Zeng, Jin J.,Rivero, Ralph A.
, p. 2230 - 2234 (2012/04/18)
A series of PI3K-beta selective inhibitors, imidazo[1,2-a]-pyrimidin-5(1H)- ones, has been rationally designed based on the docking model of the more potent R enantiomer of TGX-221, identified by a chiral separation, in a PI3K-beta homology model. Synthesis and SAR of this novel chemotype are described. Several compounds in the series demonstrated potent growth inhibition in a PTEN-deficient breast cancer cell line MDA-MB-468 under anchorage independent conditions.
