Synthesis and biological evaluation of solubilized sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474.
Basic Information
ID: ALA4480443
Journal: Bioorg Med Chem
Title: Synthesis and biological evaluation of solubilized sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474.
Authors: Giddens AC, Gamage SA, Kendall JD, Lee WJ, Baguley BC, Buchanan CM, Jamieson SMF, Dickson JMJ, Shepherd PR, Denny WA, Rewcastle GW.
Abstract: 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.
CiteXplore: 30850264
DOI: 10.1016/j.bmc.2019.02.050
Patent ID: ┄