2. Academic Validation
  3. Synthesis and activity evaluation of tilorone analogs as potential anticancer agents

Synthesis and activity evaluation of tilorone analogs as potential anticancer agents

  • Eur J Med Chem. 2013 Jun:64:432-41. doi: 10.1016/j.ejmech.2013.03.050.
Dingshan Zhou 1,  Wei Tuo,  Hao Hu,  Jianrong Xu,  Hongzhuan Chen,  Zhigang Rao,  Yuling Xiao,  Xianming Hu,  Peng Liu
Affiliations

Affiliation

  • 1 State Key Laboratory of Virology, Ministry of Education Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Wuhan University School of Pharmaceutical Sciences, Wuhan 430071, China. zhoudingshan@whu.edu.cn
PMID: 23665799 DOI: 10.1016/j.ejmech.2013.03.050
Abstract

Tilorone is an interferon inducer with Anticancer activity. Twenty-two novel tilorone analogs were synthesized by improvements of fluorenone skeleton, side chains and amino groups to screen new Anticancer agents. In vitro evaluation showed that ten new compounds had better Anticancer activities than tilorone. Among them, 2c (IC50 < 7 μM against Cancer cell lines and IC50 > 35 μM against non-cancer cell lines) and 5d (IC50 < 10 μM against Cancer cell lines and IC50 > 53 μM against non-cancer cell lines) exhibited the best Anticancer activities and selectivities. Pharmacophore modeling of highly active compounds was carried out by Molecular Operating Environment (MOE) to generate a visualized model for compound design in future study.

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