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一些取代苯并咪唑配体的铂(II)配合物的细胞毒性和 DNA 相互作用。

Cytotoxicity and DNA interactions of some platinum(II) complexes with substituted benzimidazole ligands.

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Gazi, Ankara, Turkey.

出版信息

J Enzyme Inhib Med Chem. 2012 Jun;27(3):413-8. doi: 10.3109/14756366.2011.594046. Epub 2012 Feb 3.

Abstract

In the present study, four Pt(II) complexes with 2-ethyl (1)/or benzyl (2)/or p-chlorobenzyl (3)/or 2-phenoxymethyl (4) benzimidazole carrier ligands were evaluated for their in vitro cytotoxic activities against the human HeLa cervix, oestrogen receptor-positive MCF-7 breast, and oestrogen receptor-negative MDA-MB 231 breast cancer cell lines. The plasmid DNA interactions and inhibition of the BamHI restriction enzyme activities of the complexes were also studied. Complex 3 was found to be more active than carboplatin for all examined cell lines and comparable with cisplatin, except for the HeLa cell line.

摘要

在本研究中,评估了四种具有 2-乙基(1)/或苄基(2)/或对氯苄基(3)/或 2-苯氧甲基(4)苯并咪唑载体配体的 Pt(II) 配合物的体外细胞毒性活性,针对人宫颈癌细胞系 HeLa、雌激素受体阳性 MCF-7 乳腺癌细胞和雌激素受体阴性 MDA-MB-231 乳腺癌细胞。还研究了配合物与质粒 DNA的相互作用和 BamHI 限制酶活性的抑制。与顺铂相比,除了 HeLa 细胞系外,所有检测的细胞系中,配合物 3 的活性均高于卡铂,与顺铂相当。

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