Synthesis, in vitro antimicrobial and cytotoxic activities of novel pyrimidine-benzimidazol combinations

Bioorg Med Chem Lett. 2014 Jun 15;24(12):2741-3. doi: 10.1016/j.bmcl.2014.04.037.

Peng-Ju Chen ¹, Ang Yang ¹, Yi-Fei Gu ¹, Xiao-Song Zhang ¹, Kun-Peng Shao ¹, Deng-Qi Xue ¹, Peng He ¹, Teng-Fei Jiang ¹, Qiu-Rong Zhang ², Hong-Min Liu ³

Affiliations

1 New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zhengzhou 450001, China.
2 New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zhengzhou 450001, China. Electronic address: zqr406@sina.com.
3 New Drug Research & Development Center, School of Pharmaceutical Sciences, Zhengzhou University, No. 100, KeXue DaDao, Zhengzhou 450001, China. Electronic address: liuhm@zzu.edu.cn.

PMID: 24798098 DOI: 10.1016/j.bmcl.2014.04.037

Abstract

A series of novel 4-substituted-2-{[(1H-benzo[d]imidazol-2-yl)methyl] thio}-6-methylpyrimidine derivatives were designed, synthesized and evaluated for their cytotoxic activities against four human Cancer cell lines and inhibitory activities against five type culture strains in vitro. Some of synthetic pyrimidine-benzimidazol combinations showed good inhibitory activities against Stenotrophomonas maltophilia, especially compounds 7b and 7c. Compounds 7a and 7d exhibited enhanced activities against MGC-803 in vitro, when compared to 5-Fu.

Keywords

Antimicrobial; Benzimidazole; Cytotoxic activities; Pyrimidine; Synthesis.

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