Synthesis and anticancer effects of some novel 2-(4-phenoxyphenyl)-1H-benzimidazole derivatives on K562 cell line

被引：12

作者：

Gurkan-Alp, A. Selen ^{[1
]}

Goker, Hakan ^{[1
]}

Alp, Mehmet ^{[1
]}

Ozkan, Tulin ^{[2
]}

Sunguroglu, Asuman ^{[2
]}

机构：

[1] Ankara Univ, Fac Pharm, Dept Pharmaceut Chem, TR-06100 Ankara, Turkey

[2] Ankara Univ, Fac Med, Dept Med Biol, TR-06100 Ankara, Turkey

来源：

ARCHIVES OF PHARMACAL RESEARCH | 2015年 / 38卷 / 05期

关键词：

Anticancer activity; Benzimidazole; CML; K562; Apoptosis; COMET ASSAY; BIOLOGICAL EVALUATION; INDUCED APOPTOSIS; AGENTS; 1H-BENZIMIDAZOLES; BENZIMIDAZOLES;

D O I：

10.1007/s12272-014-0438-x

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 2-(4-phenoxyphenyl)-1H-benzimidazole derivatives was synthesized and tested in vitro on human chronic myelogenous leukemia (CML) cell line K562. Benzimidazoles containing 5-amidino (10), 5-N-isopropylamidino (11), 5-bromo (13), and 5,6-dimethyl (14) derivatives exhibited remarkable cytotoxic activity. The quantitative analysis of apoptosis by flowcytometry demonstrated that the percentages of early and late apoptotic K562 cells treated with these compounds were significantly higher than cells without treatment. We also investigated the effects of these compounds on the expression of apoptosis-related genes BAX, BCL-2, BAD and BIM. Treatment of K562 cells wih compounds 10-14 significantly increased the expression levels of the proapoptotic genes BAX, BAD and BIM, whereas compound 20 increased BAX and BAD.

引用

页码：650 / 658

页数：9

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