FIELD: organic chemistry, chemical technology, medicine, pharmacy.
SUBSTANCE: invention relates to novel derivatives of varioline and their pharmaceutically acceptable salts and esters possessing anti-tumor activity. In compound of the formula (I): 
each among R1 and R2 is chosen independently from group comprising hydrogen atom (H), -OH, -OR', -SH, -SR', -SOR', -SO2R', -NO2, -NH2, -NHR', -N(R')2, -NHCOR'. -N-(COR')2, -NHSO2R', (C1-C12)-alkyl, (C1-C12)-halogenalkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic group; R3 is chosen from group comprising -OH and -OMe wherein group R' or each among groups R' is chosen independently from group comprising -OH, (C1-C12)-alkyl, (C1-C12)-halogenalkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, substituted or unsubstituted arylalkenyl and substituted or unsubstituted heteroaromatic group; if group R1 or R2 represents group of the formula -N(R')2 or -N(COR')2 then all groups R' can comprise similar or different values, either groups R' in common with nitrogen atom to which they are added can form 5-7-membered heterocyclic ring. Aryl group or aryl moiety of aralkyl and arylalkenyl group represents a carbocyclic aryl group comprising 6 carbon atoms in carbocyclic ring; aralkyl group represents (C1-C6)-alkyl group substituted with abovementioned aryl group; arylalkenyl group represents (C2-C6)-alkenyl group substituted with abovementioned aryl group; heteroaromatic group represents a heterocyclic aromatic group comprising from 5 to 7 atoms in ring wherein heteroatoms in ring are chosen from nitrogen atom; substituted in aryl and heteroaromatic groups and in aryl moiety of aralkyl and arylalkenyl groups are chosen from group comprising (C1-C12)-alkyl, (C1-C12)-halogenalkyl, (C1-C12)-alkoxy-, (C1-C12)-alkylthio-group, -NH2, (C1-C6)-alkylamino-, di-(C1-C6)-alkyl)-amino-, (C1-C4)-alkanoylamino-, di-(C1-C4)-alkanoylamino-group, -NO2, -CN and halogen atom, its derivatives wherein nitrogen atom is quaternized. Proposed compounds possess anti-tumor activity and can be used in treatment or prophylaxis of cancerous diseases, for example, ovary cancer, prostate cancer, mammary cancer and melanoma.
EFFECT: valuable medicinal properties of compounds and pharmaceutical composition, improved methods of treatment, improved methods of synthesis.
38 cl, 10 sch, 2 tbl, 25 ex
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