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Issue 7, 2015
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Synthesis, biological evaluation and mechanism study of a class of benzylideneindanone derivatives as novel anticancer agents

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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

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Supplementary files

Article information


Submitted
02 Apr 2015
Accepted
07 May 2015
First published
08 May 2015

Med. Chem. Commun., 2015,6, 1318-1327
Article type
Concise Article

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

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