Jump to main content
Jump to site search

Issue 7, 2015
Previous Article Next Article

Synthesis, biological evaluation and mechanism study of a class of benzylideneindanone derivatives as novel anticancer agents

Author affiliations

Abstract

A series of new benzylideneindanone derivatives were designed, synthesized and evaluated as antitumor agents. Structure–activity relationship (SAR) studies showed that derivatives with 4,5,6-trimethoxyl on an indanone moiety displayed good anti-proliferative activities. Especially, compound 5a demonstrated the most potent inhibitory activity, with GI50 values from 0.172 to 0.57 μM for five kinds of cancer cell lines. Further investigation showed that 5a could inhibit microtubule polymerization and thus induce G2/M phase arrest and apoptosis in A549 cells. Our findings revealed the benzylideneindanone moiety as a new attractive scaffold for mitosis-targeting drug discovery.

Graphical abstract: Synthesis, biological evaluation and mechanism study of a class of benzylideneindanone derivatives as novel anticancer agents

Back to tab navigation

Supplementary files

Publication details

The article was received on 02 Apr 2015, accepted on 07 May 2015 and first published on 08 May 2015


Article type: Concise Article
DOI: 10.1039/C5MD00139K
Citation: Med. Chem. Commun., 2015,6, 1318-1327

  •   Request permissions

    Synthesis, biological evaluation and mechanism study of a class of benzylideneindanone derivatives as novel anticancer agents

    J. Hu, J. Yan, J. Chen, Y. Pang, L. Huang and X. Li, Med. Chem. Commun., 2015, 6, 1318
    DOI: 10.1039/C5MD00139K

Search articles by author

Spotlight

Advertisements