Synthesis and Antiproliferative Activity of New Thiosemicarboxamide Derivatives |
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| Authors: | Jun Wu Yafei Guo Jun Chen Sangsang Hu Ke Sun Hongyu Hu Meijuan Fang Yuhua Xue |
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| Affiliation: | 1. Fujian Provincial Key Laboratory of Innovative Drug Target Research and State Key Laboratory of Cellular Stress Biology, School of Pharmaceutical Sciences, Xiamen University, South Xiang-An Road, Xiamen, China, 361102 These authors contributed equally to this work.;2. Fujian Provincial Key Laboratory of Innovative Drug Target Research and State Key Laboratory of Cellular Stress Biology, School of Pharmaceutical Sciences, Xiamen University, South Xiang-An Road, Xiamen, China, 361102;3. Xingzhi College, Zhejiang Normal University, Jinhua, Lanxi, 321004 China |
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| Abstract: | To discover new anticancer agents, two series of thiosemicarboxamide derivatives were synthesized and evaluated for their antiproliferative activity against human cancer cells in vitro. Most target compounds (especially 3f , 3g , and 3h ) exhibit potent antiproliferative activity against HeLa cells. Importantly, compound 3h , bearing a 4-methylphenyl substituent at N position of thiourea moiety, has significant and broad-spectrum inhibitory activities against cancer cells (HepG2, HeLa, MDA-MB231, A875, and H460 cells) with low IC50 values (<5.0 μM) and shows low toxicity to normal LO2 and MRC-5 cells. Further studies show that compound 3h exerts high inhibitory activity in cancer cells by inducing the G2/M-phase arrest of cancer cells. Collectively, this study presents compound 3h as a new entity for the development of cell cycle arrest inducers for the treatment of cancer. |
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| Keywords: | anticancer activity cell cycle structure-activity relationship thiosemicarboxamide derivative |
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