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某些苯并噻唑 - 哌嗪衍生物的细胞毒性活性。

Cytotoxic activities of some benzothiazole-piperazine derivatives.

作者信息

Gurdal Enise Ece, Durmaz Irem, Cetin-Atalay Rengul, Yarim Mine

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Yeditepe University , Kayisdagi, Istanbul , Turkey and.

出版信息

J Enzyme Inhib Med Chem. 2015;30(4):649-54. doi: 10.3109/14756366.2014.959513. Epub 2014 Oct 21.

Abstract

Synthesis, characterization and cytotoxic activities of ten benzothiazole-piperazine derivatives were reported. In vitro cytotoxic activities of compounds were screened against hepatocellular (HUH-7), breast (MCF-7) and colorectal (HCT-116) cancer cell lines by sulphorhodamine B assay. Based on the GI50 values of the compounds, most of the benzothiazole-piperazine derivatives are active against HUH-7, MCF-7 and HCT-116 cancer cell lines. Compound 1d is highly cytotoxic against all tested cancer cell lines. Further investigation of compound 1d by Hoechst Staining and Fluorescence-Activated Cell Sorting Analysis (FACS) revealed that this compound causes apoptosis by cell cycle arrest at subG1 phase.

摘要

报道了十种苯并噻唑 - 哌嗪衍生物的合成、表征及细胞毒性活性。通过磺基罗丹明B法对化合物进行体外细胞毒性活性筛选,针对肝癌细胞(HUH - 7)、乳腺癌细胞(MCF - 7)和结肠癌细胞(HCT - 116)系进行检测。根据化合物的GI50值,大多数苯并噻唑 - 哌嗪衍生物对HUH - 7、MCF - 7和HCT - 116癌细胞系具有活性。化合物1d对所有测试的癌细胞系具有高度细胞毒性。通过Hoechst染色和荧光激活细胞分选分析(FACS)对化合物1d进行的进一步研究表明,该化合物通过使细胞周期停滞在亚G1期而导致细胞凋亡。

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