CAMPTOTHECIN ANALOGS, METHODS OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 2002 - IPC

FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention relates to novel analogs of camptothecin of the formula (I) where R₁ means alkyl, alkylene, alkynyl; R₂, R₃, R₄ mean H, halogen atom, halogenalkyl, alkyl, alkenyl, -(CH₂)_mOR₆, unsubstituted or substituted phenyl or phenylalkyl; or R₃ and R₄ form in common a chain with 3-4 members that can comprise CH, CH₂, O, N or NR₉; R₃ means H, halogen atom, halogenalkyl, alkyl, alkoxy-group, substituted or unsubstituted phenyl or phenylalkyl; R₆ means H; R₉ means H, alkyl; R₁₈ and R₁₉ mean H, halogen atom, alkyl, alkoxy-group, hydroxy-group; R₂₀ means H, halogen atom; R_p means H, -C(O)-A-NR₂₂R₂₃ where A means alkylene radical; R₂₂ and R₂₃ mean H, alkyl; n = 0-6; if R_p means H then R₃ and R₄ in common form a chain with 3 or 4 members. These compounds show an inhibitory activity with respect to monoisomerase (1) and therefore they can be used as an active component in pharmaceutical composition and for its preparing. Also, the invention relates to methods of synthesis of compound of the formula (I) by interaction of compound of the formula (D) with a primary amine and by acylation of compound of the formula (D) or (Ia) with derivatives of C(O)-A-NR₂₂R₂₃. EFFECT: improved methods of synthesis, valuable biochemical properties. 13 cl, 1 tbl, 26 ex