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" Design and synthesis of formononetin-dithiocarbamate hybrids that inhibit growth and migration of PC-3 cells via MAPK/Wnt signaling pathways. "
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
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AL
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| Record Number
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901487
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| Doc. No
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LA2jw7m037
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| Title & Author
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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
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2017
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| Title of Periodical
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UC Irvine
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| Abstract
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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.
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