Design And Biological Evaluation Of DNA Intercalator Of Naphthalene Carboxamide Derivatives

A series of naphthalimide derivatives were synthesized respectively from4-bromo-l,8-napthalene anhydride and acenaphthene, and their DNA binding and anti-tumor abilities in vitro were evaluated. Also a series of benzo[c, d]indol-2(H)-one derivatives were synthesized as DNA intercalator.Four new naphthalimide derivatives were synthesized from4-bromo-l,8-napthalene, and their structure were verified by1H-NMR and mass spectrum. Their DNA binding properties were evaluated through UV-Vis spectra, fluorescence spectra and CD spectra. According to the antitumor activities test, these compounds exhibited efficient activities against MCF-7, Hela and SGC-7901cell lines. The IC50value of compound K3against MCF-7was O.13xlO-6M.6-[lH-benzo[d]imidazole-2-yl]-l,8-naphalirmides were synthesized, and their structure were verified by1H-NMR and TOF MS. The DNA binding mode was identified by spectrum researches. And the CT-DNA binding constants were calculated by Scatchard method. The results showed that all the compounds with the binding constants about104M"1can intercalate into the base pairs of DNA and transform the B-DNA to A-DNA.Series of novel benzo[c, d]indol-2(H)-one derivatives were designed and synthesized, and their structure were verified by’H-NMR and TOF MS. The EB competition experiment implied that all of compounds could intercalate into CT-DNA and their intercalation ability were stronger than EB.