CHEMICAL MODIFICATION OF ANTHRACYCLINE ANTIBIOTICS. I

DEMETHOXYCARBONYLATION, 10-EPIMERIZATION AND 4-O-METHYLATION OF ACLACINOMYCIN A

Abstract

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 on 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.