Synthesis of Phosphatidylinositol 3-Kinase (PI3K) Inhibitory Analogues of the Sponge Meroterpenoid Liphagal

[摘要]：Analogues of the sponge meroterpenoid liphagal (1) have been synthesized and evaluated for inhibition of PI3K alpha and PI3K gamma as part of a program aimed at developing new isoform-selective PI3K inhibitors. One of the analogues, compound 24, with IC50 values of 66 nM against PI3K alpha and 1840 nM against PI3K gamma, representing a 27-fold preference for PI3K alpha, exhibited enhanced chemical stability and modestly enhanced potency and selectivity compared with the natural product liphagal (1).

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