Novel indole α-methylene-γ-lactones as potent inhibitors for AKT-mTOR signaling pathway kinases

…, C Zhang, X Wu, C Yang, X Zhang, J Ding, Y Xie

Index: Ding, Huasheng; Zhang, Chao; Wu, Xihan; Yang, Chunhao; Zhang, Xiongwen; Ding, Jian; Xie, Yuyuan Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 21 p. 4799 - 4802

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Citation Number: 22

Abstract

In an effort to generate novel anticancer agents, a series of hybrids of α-methylene-γ- lactones and 2-phenyl indoles has been synthesized and evaluated for inhibition activities on the phosphorylation of AKT, mTOR, p70S6 kinase, and 4E-BP1. The results indicate that substitutes on the γ-position of lactones have a rather significant influence on inhibition activities.