NEW MATERIAL:Anthracyclines of formula I (the configuration in the 7-position is S or R; X is H or formula II).
EXAMPLE: 10-Decarbomethoxyaclacinomycin A.
USE: They have antitumorigenic activity and effectively prohibit the propagation of cultured leukemia cells and synthesis of nucleic acid even in a low concentration, thus being useful as a carcinostatic agent. They are also useful as synthetic intermediates of antitumorigenic anthracycline glycoside.
PREPARATION: Aclacinomycin A of formula III is made into an alkali aqueous solution and kept at normal temperature for a certain time. Then, a mineral acid is added to the solution to precipitate the 10-carboxyl derivative, which is separated as a powder. After the powder is brought into contact with dimethylformamide, dimethylacetamide or dimethylsulfoxide, the solvent is removed by distillation under reduced pressure or by solvent extraction. The residue is isolated by usual methods to give the compound of formula I.
YOSHIOKA TAKEO
SHIMAUCHI YASUTAKA
OKI SHIYUNICHI
INUI TAIJI
TAKEUCHI TOMIO
UMEZAWA HAMAO