Novel pyrrolo-quinoline derivatives as potent inhibitors for PI3-kinase related kinases

…, JN Sarkaria, YS Cho, RT Abraham, LH Zalkow

Index: Peng, Hairuo; Kim, Doeg-Il; Sarkaria, Jann N; Cho, Yong-Seo; Abraham, Robert T; Zalkow, Leon H Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 1 p. 167 - 174

Full Text: HTML

Citation Number: 21

Abstract

Several pyrrolo-quinoline γ-lactones were found as novel inhibitors for two members of the PI3-kinase related kinase (PIKK) family, Ataxia-Telangiectasia-mutated (ATM) protein and the mammalian Target of Rapamycin (mTOR). Preliminary structure–activity relationship studies indicated that an electrophilic exocyclic double bond conjugated to the carbonyl group of the γ-lactone ring was crucial for the PIKK inhibitory potency. One of the best ATM ...