M. Waring
Dec 1, 1976
Citations
1
Influential Citations
105
Citations
Quality indicators
Journal
European journal of cancer
Abstract
Abstract Four drugs of the 4′ -( 9 -acridinylamino) methanesulphonanilide (AMSA) series comprising the parent compound, a meta -substituted ( 3′ ) methoxy derivative and its ortho ( 2′ ) isomer, and an analogue having a 2 -methyl substituent on the acridine nucleus have been examined for effects on the supercoiled state of closed circular duplex PM 2 DNA. The parent compound and the meta -methoxy derivative are known to be highly active against L 1210 leukaemia in mice; the other two derivatives are essentially inactive. All 4 compounds were found to remove and reverse the supercoiling of PM 2 DNA consistent with the hypothesis that they bind to DNA by intercalation. Significant differences between their binding parameters and relative helix-unwinding angles were detected. The three derivatives interacted very strongly with the DNA; the parent compound less so. The helix-unwinding angle of the 2 -methyl analogue was found to be smaller than that of the other three drugs. Some, but not all, of these differences could be correlated with the antitumour activity against L 1210 cells in vivo .