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

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

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: liuhm@zzu.edu.cn.
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.

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