| 摘要 |
organic chemistry, pharmacy. SUBSTANCE: invention describes novel derivatives of camptothecin of the general formula (I) where R1 means -CH, -CH-(CN)-R4, -CH=C-(CN)-R4, -C-(= NOH)- -NH2, -C-(=NH)-NH2, -CH=C-(NO2)-R4, -CH-(CN)-R5, -CH-(CH2NO2)-R5, 5-tetrazolyl, 2-(4,5-dihydrooxazolyl), 1,2,4-oxadiazoline-3-yl-5-one; R2 means hydrogen atom; R3 means hydrogen atom, OR6; R4 means hydrogen atom, C1-C6-linear or branched alkyl, CN-group, COOR7; R5 means hydrogen atom, OR8; R6 means hydrogen atom, C1-C6-linear or branched alkyl, (C6-C12)-aryl-(C1-C4)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, (C1-C4)-alkyl-(C6-C12)-aryl, (C6-C12)-aryl-(C2-C4)-acyl, (C2-C4)-acyl, amino-(C1-C4)-alkyl, amino-(C2-C4)-acyl, glycosyl; R7 means hydrogen atom, C1-C6-linear or branched alkyl, -aryl-(C1-C4)-alkyl, (C1-C4)-alkoxy-(C1-C4)-alkyl, (C1-C4)-alkyl-(C6-C12)-aryl; R8 has the same values as R6 but independently of the latter, their N1-oxides, their isomers, diastereoisomers, enantiomers and their mixtures and active metabolites also. Compounds show antitumor activity and suitable physico-chemical properties that provide their technology of making and suitable pharmaceutical compositions. Invention describes also method of their synthesis and pharmaceutical composition. EFFECT: new compounds indicated above, improved method of synthesis, valuable antitumor activity. 16 cl, 2 tbl, 6 ex
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