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论文类型：期刊论文

发表时间：2008-07-01

发表刊物：CHEMICAL RESEARCH IN CHINESE UNIVERSITIES

收录刊物：SCIE、ISTIC、CSCD

卷号：24

期号：4

页面范围：449-453

ISSN号：1005-9040

关键字：intercalation; cytotoxicity; 8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carboxylic acid esters

摘要：To explore new platform for DNA intercalation and potent antitumor agent, a series of 8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carboxylic acid esters chromophores has been studied. Their intercalation geometries with DNA were revealed through absorption titration, SYBR Green-DNA melt curve, circular dichroism(CD), and docking studies. It was identified that some of the compounds could intercalate into DNA along their long axis parallel to the base-pair long axis, making right-handed B form DNA transform to A-like conformation. Their binding potency varied with the different steric hindrance. Their cytotoxicity(IC(50)) against MCF-7 cells was found to range between 1.3 to 40.9 mu mol/L by MTT assay. Interestingly, the IC(50) values did not show any obvious correlation to their binding constants with DNA. The chromophore with a carboxyl group exhibited the most potency of intercalating DNA and could be the promising precursor for the future intercalator for DNA, while the bromide demonstrated the highest cytotoxic activity in this series of compounds.