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某些苯并噻唑 - 哌嗪衍生物的合成与抗癌活性评估

Synthesis and anticancer activity evaluation of some benzothiazole-piperazine derivatives.

作者信息

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

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Yeditepe University, 34755, Kayisdagi, Istanbul, Turkey.

出版信息

Anticancer Agents Med Chem. 2015;15(3):382-9. doi: 10.2174/1871520615666141216151101.

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. Aroyl substituted compounds 1h and 1j were found to be the most active derivatives. In addition, further investigation of compounds 1h and 1j by Hoechst staining and FACS revealed that these compounds cause 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测定法,针对肝癌细胞(HUH - 7)、乳腺癌细胞(MCF - 7)和结肠癌细胞(HCT - 116)系筛选了化合物的体外细胞毒性活性。基于化合物的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。发现芳酰基取代的化合物1h和1j是活性最高的衍生物。此外,通过Hoechst染色和流式细胞术对化合物1h和1j进行的进一步研究表明,这些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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