Antineoplastic agents. Structure-activity relationship study of bis(substituted aminoalkylamino)anthraquinones

Abstract
A structure-activity relationship study was conducted on a number of bis(substituted aminoalkylamino)anthraquinones. These compounds were prepared by the condensation of substituted or unsubstituted leucoquinizarin with appropriate amines, followed by air oxidation. The position and the nature of the center N atom of the side chain are vital to the antineoplastic activity. The possible mode of action of these aminoquinones was discussed. 1,4-Dihydroxy-5,8-bis[[2-(hydroxyethyl)amino]ethyl]amino-9,10-anthracenedione (DHAQ) possessed potent inhibitory activity against the [mouse] P-388 leukemia system and the B-16 melanoma system.

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