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

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• 作者：Huasheng Ding ; Chao Zhang ; Xihan Wu ; Chunhao Yang ; Xiongwen Zhang ; Jian Ding and Yuyuan Xie
• 关键词：Indole α ; -methylene-γ ; -lactones ; AKT-mTOR signaling pathway kinase ; Inhibitors
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2005
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：2005
• 卷：15
• 期：21
• 页码：4799-4802
• 文件大小：151 K

摘要

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.