SEMI-SYNTHETIC ANALOGUES OF AUREOLIC ACID OLIVOMYCIN A ANTIBIOTIC, HAVING ANTI-TUMOUR ACTIVITY, AND SYNTHESIS METHOD THEREOF Russian patent published in 2012 - IPC C07H15/24 A61K31/704 A61P35/00 

Abstract RU 2453552 C2

FIELD: chemistry.

SUBSTANCE: invention relates to novel derivatives of the anti-tumour antibiotic of the aureolic acid olivomycin A group, having anti-tumour activity and low toxicity, and synthesis method thereof. The invention also relates to a method of producing derivatives of the antibiotic of the aureolic acid olivomycin A group, involving selective oxidation of the side chain of olivomycin A aglycone through reaction with sodium periodate, followed by amidation of the obtained key intermediate 1'-des-(2,3-dihydroxy-n-butyroyl)-1'-carboxyolivomycin A with corresponding amines in the presence of a condensing agent.

EFFECT: disclosed compounds have marked anti-tumour activity and low toxicity compared with the original olivomycin A.

2 cl, 9 ex, 1 dwg, 6 tbl

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RU 2 453 552 C2

Authors

Preobrazhenskaja Marija Nikolaevna

Olsuf'Eva Evgenija Nikolaevna

Tevjashova Anna Nikolaevna

Bukhman Vladimir Mikhajlovich

Shtil' Aleksandr Al'Bertovich

Dezhenkova Ljubov' Georgievna

Isakova Elena Borisovna

Maljutina Natal'Ja Mikhajlovna

Treshchalin Ivan Dmitrievich

Dates

2012-06-20Published

2010-06-18Filed