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Discovery of 3-phenylquinolinylchalcone derivatives as potent and selective anticancer agents against breast cancers.

Abstract：

:A number of 3-phenylquinolinylchalcone derivatives were synthesized and evaluated in vitro for their antiproliferative activities against three breast cancer cell lines (MCF-7, MDA-MB-231, and SKBR-3), and a non-cancer normal epithelial cell line (H184B5F5/M10). Among them, (E)-3-[3-(4-methoxyphenyl)quinolin-2-yl]-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one (7) was active against the growth of MCF-7, MDA-MB-231, and SKBR-3 with IC50 values of 1.05, 0.75, and 0.78 μM respectively without significant cytotoxicity to the normal H184B5F5/M10 cell line and therefore, was selected as a new lead for further mechanism studies. Results indicated that compound 7 inhibited the polymerization of tubulins, induced G2/M cell cycle arrest via modulation of the cyclin B1, cdk1 and CDC25. Compound 7 ultimately induced cell apoptosis by the increase of apoptotic protein Bax and the decrease of anti-apoptotic protein Bcl-2. In addition, PARP was cleaved while caspase-3 and -8 activities were induced after the treatment of compound 7 for 24 h in a concentration-dependent manner. Thus, compound 7 induces cell cycle arrest at G2/M phase via cleavage of PARP, induces caspase-3 and -8 activities and consequently to cause the cell death. Further study on the structure optimization of 7 is ongoing.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Tseng CH,Tzeng CC,Hsu CY,Cheng CM,Yang CN,Chen YL

doi

10.1016/j.ejmech.2015.04.054

subject

Has Abstract

pub_date

2015-06-05 00:00:00

pages

306-19

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(15)30018-0

journal_volume

97

pub_type

杂志文章

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