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

Huasheng Ding, Chao Zhang, Xihan Wu, Chunhao Yang, Xiongwen Zhang, Jian Ding, Yuyuan Xie

Research output: Contribution to journalArticlepeer-review

23 Scopus citations

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.

Original languageEnglish
Pages (from-to)4799-4802
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number21
DOIs
StatePublished - 1 Nov 2005
Externally publishedYes

Keywords

  • AKT-mTOR signaling pathway kinase
  • Indole α-methylene-γ-lactones
  • Inhibitors

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