Structure-activity relationship study of anthraquinones:...

An oxygen analog of the antineoplastic anthraquinone, 1,4-dihydroxy-5,8-bis[[2-(2-hydroxyethyl)amino]ethyl]amino - 9,10-anthracenedione, was synthesized. This compound, 1,4-dihydroxy-5,8-bis[[2-(2-hydroxyethoxy)ethyl]amino] - 9,10-anthracenedione, was found to be inactive against P-388 lymphocytic leukemia. A comparative structure-activity study of these two anthraquinones in terms of previously postulated N--O--O triangulation hypothesis was discussed.