Synthesis, Crystal Structure and Biological Activity of 2-[(Pyridin-2-yl)methylthio]-1H-benzimidazole Derivatives

Subjects: Chemistry >> Physical Chemistry submitted time 2017-11-05 Cooperative journals: 《结构化学》

GAO Di CHEN Gu-Zhou CAO Sheng DU Yue JIN Zhe LIU Xiao-Ping OUYANG Gui-Ping HU Chun

Abstract： In order to discover the novel anti-tumor agents, a series of 2-[(pyridin-2-yl)methylthio]-1H-benzimidazole derivatives were designed and synthesized, and the structures were characterized by IR, MS, and proton NMR. 2-[(3,4-Dimethoxypyridin-2-yl)methylthio]-1H-benzimidazole was investigated with X-ray crystallography, and the molecule is in orthorhombic system, space group P212121, with a = 9.1828(16), b = 11.625(2), c = 13.463(2) � Z = 4, R = 0.0231 and wR = 0.0596. The antitumor activities of target compounds were evaluated against human liver cancer cell line HepG2, and human liver normal cell line HL7702 using MTT assay. The target compounds have demonstrated weak or moderate anti-tumor activity against HepG2, while all the target compounds exhibit no cytotoxic effects on HL7702.

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