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A new ionizable chromophore of 1,4-bis(alkylamino)benzo[g]phthalazine which interacts with DNA by intercalation

AuthorsPons, Miquel; Campayo, Lucrecia; Martínez-Balbás, Marian ; Azorín, Ferran ; Navarro, Pilar ; Giralt, Ernest
Issue Date1991
PublisherAmerican Chemical Society
CitationJournal of Medicinal Chemistry 34(1):82-86 (1991)
AbstractThe tricyclic heteroaromatic nucleus of 1,4-bis(alkylamino)benzo[g]phthalazine can be protonated at physiological pH, depending on the nature of the side chains. The interaction of the 3-methoxypropyl derivative with calf thymus and closed, circular DNA has been studied with UV-vis spectroscopy and NMR. The effect of drug binding on the topology of closed, circular DNA was determined by topoisomerase-I catalyzed relaxation of the complex followed by gel electrophoresis. The results strongly support intercalative binding and suggest that this series of compounds are promising targets for anticancer activity evaluation. © 1991 American Chemical Society
Publisher version (URL)http://dx.doi.org/10.1021/jm00105a014
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