Synthesis and biological evaluation of benzofuran-based 3,4,5-trimethoxybenzamide derivatives as novel tubulin polymerization inhibitors.

Abstract:

:A new series of derivatives characterized by the presence of the 3,4,5-trimethoxylbenzamide substituted benzofurans were synthesized and evaluated for antiproliferative activity against four cancer cell lines and one normal human cell line. Among them, derivative 6g with greatest cytotoxicity significantly inhibited the growth of MDA-MB-231, HCT-116, HT-29 and HeLa cell lines with IC50 values of 3.01, 5.20, 9.13, and 11.09 μM, respectively. Importantly, 6g possessed excellent selectivity over non-tumoral cell lines HEK-293 (IC50 > 30 μM). Moreover, mechanistic studies revealed that 6g induced HeLa cells arrested in G2/M phase in a concentration-dependent manner, and inhibited polymerization of tubulin via a consistent way with CA-4. In general, these observations suggest that 6g is a promising anti-cancer lead and is worth further investigation to generate potential antitumor agents.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Li Q,Jian XE,Chen ZR,Chen L,Huo XS,Li ZH,You WW,Rao JJ,Zhao PL

doi

10.1016/j.bioorg.2020.104076

subject

Has Abstract

pub_date

2020-09-01 00:00:00

pages

104076

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(20)31373-0

journal_volume

102

pub_type

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