2. Academic Validation
  3. Acylhydrazone derivatives as potential anticancer agents: Synthesis, bio-evaluation and mechanism of action

Acylhydrazone derivatives as potential anticancer agents: Synthesis, bio-evaluation and mechanism of action

  • Bioorg Med Chem Lett. 2015 Dec 15;25(24):5772-6. doi: 10.1016/j.bmcl.2015.10.069.
Xifang Yu 1,  Liqiao Shi 2,  Shaoyong Ke 3
Affiliations

Affiliations

  • 1 Huangshi Central Hospital, Hubei Polytechnic University, Huangshi 435000, People's Republic of China.
  • 2 National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, People's Republic of China.
  • 3 National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, People's Republic of China. Electronic address: keshaoyong@163.com.
PMID: 26546214 DOI: 10.1016/j.bmcl.2015.10.069
Abstract

A series of novel acylhydrazone derivatives were designed, synthesized and evaluated for their potential cytotoxic effects against human Cancer cell lines. The preliminary results indicated that some of the obtained compounds (such as 8b, 13c) exhibited good to moderate cytotoxic activities against human HepG2, Huh-7, and BCG-823 cell lines. Especially, compounds 8c and 8e presented obviously selective cytotoxic activities against Huh-7 in vitro (8c, IC50=7.74±2.18μg/mL; 8e, IC50=4.46±1.05μg/mL) compared to 5-FU (IC50=10.41±3.41μg/mL). The highly potential compounds to induce Apoptosis in HepG2 cells were analyzed by flow cytometry, and the apoptotic effects of compounds 8b and 13c were further evaluated using Annexin V-FITC/propidium iodide dual staining assay.

Keywords

Acylhydrazone; Apoptosis; Cytotoxic activity; Synthesis.

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