Synthesis and biological evaluation of novel pyrimidine-benzimidazol hybrids as potential anticancer agents

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3877-81. doi: 10.1016/j.bmcl.2014.06.050.

Kun-Peng Shao ¹, Xu-Yao Zhang ¹, Peng-Ju Chen ¹, Deng-Qi Xue ¹, Peng He ¹, Li-Ying Ma ¹, Jia-Xin Zheng ¹, Qiu-Rong Zhang ², Hong-Min Liu ³

Affiliations

1 School of Pharmaceutical Sciences and New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, PR China.
2 School of Pharmaceutical Sciences and New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, PR China. Electronic address: zqr406@sina.com.
3 School of Pharmaceutical Sciences and New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, PR China. Electronic address: liuhm@zzu.edu.cn.

PMID: 25001482 DOI: 10.1016/j.bmcl.2014.06.050

Abstract

A series of pyrimidine-benzimidazol hybrids was synthesized and evaluated for Anticancer activity on four human Cancer cell lines including MCF-7, MGC-803, EC-9706 and SMMC-7721. Some of the synthesized compounds exhibited moderate to potent activity against MGC-803 and MCF-7. Among them, compounds 5a-b and 6a-b showed most effective activity. Compounds 5b and 6b were more cytotoxic than 5-fluorouracil against all tested four human Cancer cell lines, with IC50 values ranging from 2.03 to 10.55 μM and 1.06 to 12.89 μM, respectively. Flow cytometry analysis demonstrated that treatment of MGC-803 with 6b led to cell cycle arrest at G2/M phase accompanied by an increase in apoptotic cell death.

Keywords

Anticancer; Apoptosis; Benzimidazole; Cell cycle arrest; Pyrimidine.

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