Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).

doi:10.1021/jm200688y

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Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).

Journal of medicinal chemistry - 27 Oct 2011

Rewcastle Gordon W, Gamage Swarna A, Flanagan Jack U, Frederick Raphael, Denny William A, Baguley Bruce C, Kestell Philip, Singh Ripudaman, Kendall Jackie D, Marshall Elaine S, Lill Claire L, Lee Woo-Jeong, Kolekar Sharada, Buchanan Christina M, Jamieson Stephen M F, Shepherd Peter R

Abstract excerpt

A structure-activity relationship (SAR) study of the pan class I PI 3-kinase inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474) identified substitution at the 4 and 6 positions of the benzimidazole ring as having significant effects on the potency of substituted derivatives. The 6-amino-4-methoxy analogue displayed a greater than 1000-fold potency enhancement over...

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PMID: 21882832
DOI: 10.1021/jm200688y

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