Synthesis and biological evaluation of sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474.

作者: Swarna A Gamage , Anna C Giddens , Kit Y Tsang , Jack U Flanagan , Jackie D Kendall

DOI: 10.1016/J.BMC.2017.09.025

关键词:

摘要: Replacing one of the morpholine groups phosphatidylinositol 3-kinase (PI3K) inhibitor ZSTK474 with a variety sulfonamide-linked solubilizing substituents produced new class active and potent PI3Kα inhibitors, several derivatives demonstrating high enzyme potency good cellular in two human derived cell lines. The overall results suggest preference for linear somewhat flexible functions. From this series, compound 16, also known as SN32976, was selected advanced preclinical evaluation.

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