Synthesis and Antiproliferative Activity of New Thiosemicarboxamide Derivatives

  • Chem Biodivers. 2021 Dec;18(12):e2100671. doi: 10.1002/cbdv.202100671.
Jun Wu  1 ,  Yafei Guo  1 ,  Jun Chen  1 ,  Sangsang Hu  2 ,  Ke Sun  1 ,  Hongyu Hu  2  3 ,  Meijuan Fang  1 ,  Yuhua Xue  1
Affiliations
  • 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.
  • 2. Xingzhi College, Zhejiang Normal University, Jinhua, Lanxi, 321004, China.
  • 3. Key Laboratory of the Ministry of Education for Advanced Catalysis Materials, Zhejiang Normal University, Jinhua, 321004, China.
PMID: 34738709 DOI: 10.1002/cbdv.202100671
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.

Keywords
anticancer activity; cell cycle; structure-activity relationship; thiosemicarboxamide derivative.
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