A number of unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones have been synthesized and evaluated for their antitumor activity against L1210 in vitro and in vivo. The high activity of several compounds observed in vitro was not paralleled by comparable activity in vivo. The activities of the substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones as inhibitors of cell growth were generally much higher than those of the related 1-[(aminoalkyl)amino]-4-methoxyanthracene-9,10-diones, and this correlated with the relative abilities of compounds of the two types to interact with calf thymus DNA.
Several 5,8-bis[(aminoalkyl)amino]-1-azaanthracene-9,10-diones have been synthesized and evaluated for antitumor activity against L1210 leukemia both in vitro and in vivo. Comparisons are made to the corresponding carbocyclic analogues. One of the aza analogues showed modest in vivo activity.
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