1246203-83-7Relevant articles and documents
Synthesis and biological evaluation of solubilized sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474
Giddens, Anna C.,Gamage, Swarna A.,Kendall, Jackie D.,Lee, Woo-Jeong,Baguley, Bruce C.,Buchanan, Christina M.,Jamieson, Stephen M.F.,Dickson, James M.J.,Shepherd, Peter R.,Denny, William A.,Rewcastle, Gordon W.
, p. 1529 - 1545 (2019/03/07)
Replacing one of the morpholine groups of the phosphatidylinositol 3-kinase (PI3K) inhibitor ZSTK474 with a variety of sulfonamide-linked solubilizing substituents produced a new class of active and potent PI3Kα inhibitors, with several derivatives demonstrating high PI3Kα enzyme potency and good cellular potency in two human derived cell lines. The overall results suggest a preference for linear and somewhat flexible solubilizing functions. From this series, compound 16, also known as SN32976, was selected for advanced preclinical evaluation.