AI Article Synopsis
- * These new compounds showed strong potency against the PI3Kα enzyme and performed well in human-derived cell lines.
- * Among the new derivatives, compound 16 (SN32976) was chosen for further preclinical testing due to its effectiveness.
Article 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.
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| http://dx.doi.org/10.1016/j.bmc.2019.02.050 | DOI Listing |
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