[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. The use of physicochemical methods showed that the chemical modification involved the primary and secondary amino groups++ of spermidine++ and gave rise to N,N'-diacyl, N,N'-dicarbamoyl and N,N'-dialkyl bleomycetins. The biological properties of the derivatives, i.e. their cytotoxic activity, acute and pulmonary toxicities were studied. The transformation of bleomycetin by the C-end fragment lowered the antibiotic toxicity and was believed to be a promising approach to modifying its molecule.
D000215:Acylation; D000478:Alkylation; D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D001761:Bleomycin / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use / Q000031:analogs & derivatives; D002850:Chromatography, Gel / Q000379:methods; D004353:Drug Evaluation, Preclinical; D066298:In Vitro Techniques; D007942:Leukemia, Experimental / Q000188:drug therapy*; D007945:Leukemia, Lymphoid / Q000188:drug therapy*; D051379:Mice; D011199:Potentiometry / Q000379:methods; D013056:Spectrophotometry, Ultraviolet / Q000379:methods; D013095:Spermidine / Q000138:chemical synthesis* / Q000737:chemistry
D000903:Antibiotics, Antineoplastic; D001761:Bleomycin; C025703:bleomycetin; D013095:Spermidine
Khimicheskaia modifikatsiia protivoopukholevogo antibiotika bleomitsetina po C-kontsevomu fragmentu.