1-氮杂苯并蒽酮-吖啶类似物杂合体与DNA的相互作用及其抗肿瘤活性的研究
Hybrids of 1-azabenzanthrone-acridine congeners:DNA binding affinity and it's antitumor activity
作者:唐煌;戴支凯;赵丽珍;吴玉环;陈振锋;
Author:
收稿日期: 年卷(期)页码:2012,27(05):-482-485
期刊名称:华西药学杂志
Journal Name:WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字:1-氮杂苯并蒽酮衍生物;DNA结合;抗肿瘤
Key words:
基金项目:国家自然科学基金资助项目(批准号:20861002);;
广西自然科学基金(桂科自0832095);;
广西“八桂学者”计划资助;;
广西师范大学博士后启动基金资助
中文摘要
目的研究合成的1-氮杂苯并蒽酮-吖啶类似物杂合体(Ia~Il)与小牛胸腺DNA的相互作用及抗肿瘤活性。方法利用紫外吸收光谱、荧光光谱研究杂合体与小牛胸腺DNA的相互作用;用MTT法评价杂合体对人肺腺癌(SPC-A)、人宫颈癌(Hela)、人肝癌(HepG2)、人胃癌(SGC-7901)、人肺癌(NCI-H460)、人结直肠癌(SW480)和人肾腺癌(786-O)等7种肿瘤细胞株的毒性。结果杂合体能与小牛胸腺DNA发生嵌入结合作用,细胞毒性测试表明杂合体具有较强的抗肿瘤活性,特别是对SGC-7901、NCI-H460、SW480和786-O等细胞系的毒性最强,其中大部分杂合体的IC50
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