Chemical modification of anthracycline antibiotics. I. Demethoxycarbonylation, 10-epimerization and 4-o-methylation of aclacinomycin A.

Demethoxycarbonyl derivatives of aclacinomycin A and of its 7-epimer, 10-epi-aclacinomycin A and 4-O-methylaclacinomycin A were chemically derived from aclacinomycin A. The cytotoxicity and inhibitory effects of RNA and DNA synthesis in cultured L1210 leukemia cells of the 4-O-methyl derivative approximated that of aclacinomycin A, while the demethoxycarbonyl derivatives and 10-epi-aclacinomycin A exhibited decreased activities in comparison with the parent compound.