Analogs of sandramycin (1) are synthesized and shown to have cytoxicity against various tumor cell types. The relative cytotoxic properties of the sandramycin analogs are approximately parallel tp their relative DNA binding affinities. An exception to this generalization is compound (4) which completely the sandramycin chromophore phenol. Although typically 4-10.times. less potent than sandramycin against leukemia cell lines, compound (4) proved to be 1-10,000.times. more potent against melanomas, carcinomas, and adenocarcinomas exhibiting IC.sub.50 values of 1 pM-10 nM. This activity places compound (4) amongst the most potent agents identified to date.