Barbara Stefanska

Synthesis, antileukemic evaluation and peroxidating ability of heterosubstituted anthracene-9,10-dione analogues: 5,8-[(aminoalkyl)amino]naphtho[2,3-d]thiazole-4,9-diones and 5,8-[(aminoalkyl)amino]naphtho[2,3-c] [1,2,5]thiadiazole-4,9-diones

Abstract The syntheses of a number of heterosubstituted ametantrone analogues, 5,8-bis[(aminoalkyl)amino]naphtho[2,3- d ]thiazole-4,9-diones and 5,8-bis[(aminoalkyl)amino]naphtho[2,3- c ] [1,2,5]thiadiazole-4,9-diones, have been performed. It was evidenced that this modification in the chromophore moiety has a negative effect on antileukemic activity. This modification also favors the affinity of the compounds toward NADH dehydrogenase and influences the redox potential.

Synthesis and antineoplastic evaluation of N-enamine derivatives of 1,4-bis[(2-aminoethyl)amino]-9,10-anthracenedione

Abstract Several N -enamine derivatives of 1,4-bis[(2-aminoethyl)amino]-9,10-anthracenedione have been synthesized in the reaction of 1,4-bis[(2-aminoethyl)amino]-9,10-anthracenedione with various β-dicarbonyl compounds. The obtained derivatives exhibited cytotoxicity in vitro comparable or lower to that of ametantrone but their in vivo activity against P388 murine leukemia was decreased.