Design, synthesis and evaluation of novel indole derivatives as AKT inhibitors

D Yang, P Wang, J Liu, H Xing, Y Liu, W Xie…

Index: Yang, Dezhi; Wang, Peng; Liu, Jianzhen; Xing, Hualu; Liu, Yang; Xie, Wencheng; Zhao, Guisen Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 1 p. 366 - 373

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Citation Number: 4

Abstract

Abstract Herein, we describe the discovery and synthesis of a new series of 1, 2, 4, 7-tetra- substituted indole derivatives as novel AKT inhibitors by optimization of a weak hit methyl 4- (2-aminoethoxy)-1H-indole-2-carboxylate (1). Both representative compounds 6a and 6o exhibited the most potent inhibitory activities against AKT1, with inhibition rates of 72.5% and 78.6%, respectively, at concentrations of 10 nM. In addition, compounds 6a and 6o ...