[Reaction of acylation of the antineoplastic antibiotic bleomycetin].

The reaction of benzoylation of bleomycetin, a glycopeptide antibiotic, and its cuprum complex was studied with the chloranhydride and carbodiimide methods. Acylation of the antibiotic cuprum complex by an equivalent quantity of benzoyl chloride resulted in formation of a mixture of mono- and disubstituted derivatives while with the use of a 3-fold excess of chloranhydride it was possible to obtain dibenzoylbleomycetin as a sole reaction product. Interaction of the bleomycetin cuprum complex with activated benzoic ether resulted in formation of a product monosubstituted by the antibiotic spermidine fragment.

[Chemical modification of an antineoplastic antibiotic bleomycetin by the C-end fragment].

Bleomycetin, an antitumor antibiotic, was subjected to chemical modification by the C-end fragment i.e. the residue of 3-[(4-aminobutyl)amino]propylamine (spermidine++) with acylation, carbamoylation and reducing alkylation, which yielded its new semisynthetic derivatives.