2,5-Diamino-1,4-naphthoquinone Imineのデオキシリボ核酸との相互作用ならびにその生物活性

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The interaction of synthetic aminoquinone derivative, 2,5-diamino-1,4-naphthoquinone imine (DANQI), with calf thymus deoxyribonucleic acid (DNA) in vitro in a ratio of up to 1 mol to two nucleotide residues with the binding constant of 3.9×10^3 M^<-1> was confirmed by spectrometric and melting experiments, and by equilibrium dialysis. The three sites in DNA assumed to take part in this interaction are the adenine base, the 2'-deoxycytidine residue, and possibly the phosphodiester bond. Although the mode of this interaction was somewhat different from those for both 2-amino-1,4-naphthoquinone imine (ANQI) and 2-hydroxyamino-1,4-naphthoquinone (HANQ), which interacted with DNA at the adenine and the guanine bases, DANQI inhibited the DNA synthesis, possibly as the primary action, in Ehrlich ascites carcinoma cells in vitro in the same manner as the above two derivatives. The extent of inhibition by DANQI in the carcinoma cells was greater than that by mitomycin C and was also greater than that in E. coli. The difference in the biological activities between the hydroxyamino (HANQ) and the amino (DANQI and ANQI) derivatives was that the former had a therapeutic effect on Ehrlich mouse ascites carcinoma in vivo, while the latter did not.
1977-09-25