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, …
GW Rewcastle, SA Gamage, JU Flanagan…
文献索引：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. Journal of Medicinal Chemistry, 2011 , vol. 54, # 20 p. 7105 - 7126
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]-1 H-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 the corresponding 6-aza-4 ...
