摘要:
Novel antibiotics cleomycins represented by the formula ##STR1## wherein R is a terminal amino residue of the cleomycin. These compounds are useful as a chemotherapeutic agent for treating cancer and bacterial infections.
摘要:
Novel 3-[(S)-1'-phenylethylamino]propylaminobleomycin obtained by reacting a reactive derivative of the carboxyl group of bleomycinic acid with N-[(S)-1'-phenylethyl]-1,3-diaminopropane, a non-toxic salt of said novel bleomycin, and a method for producing the novel bleomycin. Because of much reduction in the side effect causing pulmonary fibrosis, the novel bleomycin is more useful than a commercial bleomycin complex which gives rise to said undesirable side effect.
摘要:
This invention is concerned with the oxidative conversion of an unstable phleomycin group to a stable bleomycin group antibiotic having the partial structure: ##SPC1##By treatment with potassium ferricyanide or manganese dioxide.
摘要:
N-methylbleomycins represented by the general formula ##STR1## which are useful as antitumor agents and bactericides; a method of preparing the same; and intermediate products in the preparation thereof.
摘要:
Novel 3-[(S)-1'-phenylethylamino]propylaminobleomycin obtained by reacting a reactive derivative of the carboxyl group of bleomycinic acid with N-[(S)-1'-phenylethyl]-1,3-diaminopropane, a non-toxic salt of said novel bleomycin, and a method for producing the novel bleomycin. Because of much reduction in the side effect causing pulmonary fibrosis, the novel bleomycin is more useful than a commercial bleomycin complex which gives rise to said undesirable side effect.
摘要:
By adding a specific amine in culturing under aerobic conditions actinomycetales capable of producing phleomycin group antibiotics, which have been inoculated into a nutrient medium to produce antitumor phleomycin group antibiotics, it is possible to obtain specific phleomycin group antibiotics having a side chain structure corresponding to said amine. The phleomycin group antibiotics thus produced are collected from the culture medium in a conventional way.
摘要:
A novel process for producing antibiotics bleomycins by innoculating and aerobically culturing in a nutrient source-containing medium a bleomycin-producing strain belonging to the actinomyces, wherein the culture is effected in the presence of an amino compound having at least one ##STR1## group and at least one basic group selected from amino, imino, guanidino, amidino and sulfonium groups and nitrogen-containing cyclic compounds, or in the presence of a compound convertible in the culture liquor to such amino compound as mentioned above, thereby selectively producing a known or novel bleomycin component corresponding to the said amino compound or to an amino compound derived from the above-mentioned compound, and then the known or novel bleomycin is recovered by known means from the culture medium.
摘要:
By thermal decomposition of 3-(S,S-dimethylmercapto)propylaminobleomycin, there is easily obtained 3-(methylmercapto)propylaminobleomycin which is a useful antibiotic substance having an extremely high antimicrobial activity and a carcinostartic activity with low toxicity.
摘要:
Disclosed is a 3-(4'-aminobutylamino) propylaminobleomycin having low pulmonary toxicity, which expressed by the following general formula[BX]--NH--(CH.sub.2).sub.3 --A--(CH.sub.2).sub.4 --Bwherein [BX] represents a residue remaining after removing a hydroxyl group from the carboxyl group of bleomycinic acid, A represents a group of the formula ##STR1## in which R.sub.1 represents (i) a hydrogen atom, (ii) an alkyl group having 1 to 10 carbon atoms, or (iii) a methyl which may be substituted by at least one of a phenyl group and a cycloalkyl group having 5 to 13 carbon atoms, said substituents being each optionally further substituted more than one position by one or more substituents selected from the class consisting of a halogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms, and benzyloxy group; and R.sub.2 represents a lower alkyl group having 1 to 4 carbon atoms or a benzyl group, B represents a group of the formula ##STR2## in which R.sub.3 and R.sub.4 each represents (i) a hydrogen atom, (ii) an alkyl group having 5 to 10 carbon atoms, or (iii) a methyl which may be substituted by at least one of a phenyl group and a cycloalkyl group, said substituents being each optionally further substituted more than one position by one or more substituents selected from the class consisting of a halogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms and a benzyloxy group, with the proviso that at least one of R.sub.3 and R.sub.4 is a group other than a hydrogen atom, and salt thereof.
摘要:
An aminopropylaminobleomycin represented by the following formula or a salt thereof, which is minimized in side effects such as pulmonary toxicity:[BX]--NH--(CH.sub.2).sub.3 --A--)CH.sub.2).sub.3 --Bwherein[BX] represents the acyl group of bleomycinic acid whose formula differs from that of bleomycin acid by the removal of the hydroxyl group from the carboxyl group of said acid;A represents a group of the general formula ##STR1## wherein R.sub.1 is a lower alkyl or benzyl,R.sub.2 is a lower alkyl or benzyl,R is a lower alkylene, andn is 0 or 1; andB represents a group of the formula ##STR2## wherein (i) R.sub.3 is hydrogen and R.sub.4 is(a) benzyl substituted by one or more halogen atoms, provided that the benzyl is substituted by two halogen atoms when R.sub.1 is lower alkyl,(b) benzyl substituted by cyano, two or more alkoxy groups or two or more benzyloxy groups,(c) lower alkyl substituted by cycloalkyl or anthranyl,(d) phenylethyl substituted by one or more halogen atoms, or(e) diphenylethyl; or(ii) both R.sub.3 and R.sub.4 are benzyl which may be substituted by one or more(a) benzyloxy groups,(b) ring substituted benzyloxy groups in which the ring substituents may be one or more halogen atoms, lower alkoxy groups or benzyloxy groups, or(c) cycloalkylmethoxy groups;and a process for the preparation thereof.