Discovery of N-(4-methoxyphenyl)-N, 2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier …

…, S Kasibhatla, B Tseng, J Drewe, SX Cai

Index: Sirisoma, Nilantha; Pervin, Azra; Zhang, Hong; Jiang, Songchun; Willardsen, J. Adam; Anderson, Mark B.; Mather, Gary; Pleiman, Christopher M.; Kasibhatla, Shailaja; Tseng, Ben; Drewe, John; Cai, Sui Xiong Journal of Medicinal Chemistry, 2009 , vol. 52, # 8 p. 2341 - 2351

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Citation Number: 89

Abstract

As a continuation of our structure− activity relationship (SAR) studies on 4- anilinoquinazolines as potent apoptosis inducers and to identify anticancer development candidates, we explored the replacement of the 2-Cl group in our lead compound 2-chloro- N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (6b, EP128265, MPI-0441138) by other functional groups. This SAR study and lead optimization resulted in the identification of N-( ...