2. Academic Validation
  3. Synthesis, antitumor activity and mechanism of action of novel 1,3-thiazole derivatives containing hydrazide-hydrazone and carboxamide moiety

Synthesis, antitumor activity and mechanism of action of novel 1,3-thiazole derivatives containing hydrazide-hydrazone and carboxamide moiety

  • Bioorg Med Chem Lett. 2016 Jul 15;26(14):3263-3270. doi: 10.1016/j.bmcl.2016.05.059.
Haifeng He 1,  Xiaoyan Wang 1,  Liqiao Shi 2,  Wenyan Yin 2,  Ziwen Yang 2,  Hongwu He 3,  Ying Liang 4
Affiliations

Affiliations

  • 1 Key Laboratory of Pesticide and Chemical Biology of Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, China.
  • 2 National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, China.
  • 3 Key Laboratory of Pesticide and Chemical Biology of Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, China. Electronic address: he1208@mail.ccnu.edu.cn.
  • 4 National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, China. Electronic address: liangying2004123@163.com.
PMID: 27262600 DOI: 10.1016/j.bmcl.2016.05.059
Abstract

A series of novel 2,4,5-trisubstituted 1,3-thiazole derivatives containing hydrazide-hydrazine, and carboxamide moiety including 46 compounds T were synthesized, and evaluated for their antitumor activity in vitro against a panel of five human Cancer cell lines. Eighteen title compounds T displayed higher inhibitory activity than that of 5-Fu against MCF-7, HepG2, BGC-823, Hela, and A549 cell lines. Especially, T1, T26 and T38 exhibit best cytotoxic activity with IC50 values of 2.21μg/mL, 1.67μg/mL and 1.11μg/mL, against MCF-7, BCG-823, and HepG2 cell lines, respectively. These results suggested that the combination of 1,3-thiazole, hydrazide-hydrazone, and carboxamide moiety was much favorable to cytotoxicity activity. Furthermore, the flow cytometry analysis revealed that compounds T1 and T38 could induce Apoptosis in HepG2 cells, and it was confirmed T38 led the induction of cell Apoptosis by S cell-cycle arrest.

Keywords

1,3-Thiazole; Antitumor activity; Apoptosis; Carboxamide; Hydrazide–hydrazone.

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