Design and synthesis of novel 1,2,3-triazole-pyrimidine hybrids as potential anticancer agents

  • Eur J Med Chem. 2014 Oct 30:86:368-80. doi: 10.1016/j.ejmech.2014.08.010.
Li-Ying Ma  1 ,  Lu-Ping Pang  1 ,  Bo Wang  1 ,  Miao Zhang  1 ,  Biao Hu  1 ,  Deng-Qi Xue  1 ,  Kun-Peng Shao  1 ,  Bao-Le Zhang  1 ,  Ying Liu  1 ,  En Zhang  1 ,  Hong-Min Liu  2
Affiliations
  • 1. New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China.
  • 2. New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, Avenue Kexue, Zhengzhou 450001, PR China. Electronic address: [email protected].
PMID: 25180925 DOI: 10.1016/j.ejmech.2014.08.010
Abstract

A series of novel 1,2,3-triazole-pyrimidine hybrids were designed, synthesized and evaluated for their Anticancer activity against four selected Cancer cell lines (MGC-803, EC-109, MCF-7 and B16-F10). Most of the synthesized compounds exhibited moderate to good activity against all the Cancer cell lines selected. Compound 17 showed the most excellent Anticancer activity with single-digit micromolar IC50 values ranging from 1.42 to 6.52 μM. Further mechanism studies revealed that compound 17 could obviously inhibit the proliferation of EC-109 Cancer cells by inducing Apoptosis and arresting the cell cycle at G2/M phase.

Keywords
Anticancer; Apoptosis; Cell cycle arrest; Pyrimidine; Triazole.