عنوان
پدید آورنده
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رده
کتابخانه
محل استقرار
LA2jw7m037
Design and synthesis of formononetin-dithiocarbamate hybrids that inhibit growth and migration of PC-3 cells via MAPK/Wnt signaling pathways.
[Article]
Fu, Dong-JunZhang, LiSong, JianMao, Ruo-WangZhao, Ruo-HanLiu, Ying-ChaoHou, Yu-HuiLi, Jia-HuanYang, Jia-JiaJin, Cheng-YunLi, PingZi, Xiao-LinLiu, Hong-MinZhang, Sai-YangZhang, Yan-Bing
A series of novel formononetin-dithiocarbamate derivatives were designed, synthesized and evaluated for antiproliferative activity against three selected cancer cell line (MGC-803, EC-109, PC-3). The first structure-activity relationship (SAR) for this formononetin-dithiocarbamate scaffold is explored in this report with evaluation of 14 variants of the structural class. Among these analogues, tert-butyl 4-(((3-((3-(4-methoxyphenyl)-4-oxo-4H-chromen-7-yl)oxy)propyl)thio)carbonothioyl)piperazine-1-carboxylate (8i) showed the best inhibitory activity against PC-3 cells (IC 50 = 1.97 μM). Cellular mechanism studies elucidated 8i arrests cell cycle at G1 phase and regulates the expression of G1 checkpoint-related proteins in concentration-dependent manners. Furthermore, 8i could inhibit cell growth via MAPK signaling pathway and inhibit migration via Wnt pathway in PC-3 cells.
2017
UC Irvine
مطالعه متن کتاب [Article]
277837
a
Y
