CARBOCYCLIC ANALOGS OF 20(S)-CAMPTOTHECIN, METHODS OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT

摘要

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to novel water-soluble C-cyclic analogs of 20(S)-camptothecin of the general formula (1) or their pharmaceutically acceptable salts where R¹, R², R³, R⁴ mean independently H, OH, C₁-C₈-alkoxy-group, NO₂-group, substituted NH₂,-group containing one or two substituted taken among C₁-C₆-alkyl, halogen-C₁-C₆-alkyl, C₁-C₆-alkyl, substituted C₁-C₆-alkyl; R⁵ is H, C₁-C₆-alkyl; R⁶ is H, C₁-C₆-alkyl, benzyl that can be substituted, substituted benzoyl, substituted C₁-C₆-alkyl; in the case when NH₂-group is bisubstituted then substitutes can be combined to form heterocyclic ring containing 5-7 carbon atoms and 1 or 2 nitrogen atoms and oxygen atom optionally. Compounds show strong anticancer and antiviral properties. All compounds are synthesized from compounds of the general formula (2) containing chiral carbon atom 20(S) where substituted R¹-R⁵ have the above indicated values. EFFECT: improved method of synthesis, valuable medicinal properties of compounds. 14 cl, 4 tbl