C7-ESTER-SUBSTITUTED TAXANES AS ANTI-TUMOR AGENTS Russian patent published in 2005 - IPC

FIELD: organic chemistry of natural compounds, medicine, oncology.

SUBSTANCE: invention relates to new compounds - C7-ester-substituted taxanes of the general structural formula:

wherein R₂ represents benzoyloxy-group; R₇ represents R_7aCOO-; R₁₀ represents hydroxy-group; X₃ represents (C₁-C₈)-alkyl, (C₂-C₈)-alkenyl, (C₂-C₈)-alkynyl or 5- or 6-membered heteroaryl group comprising heteroatom taken among oxygen (O), nitrogen (N) and sulfur (S) atoms; X₅ represents -COX₁₀ wherein X₁₀ represents (C₁-C₈)-alkyl, (C₂-C₈)-alkenyl, phenyl or 5- or 6-membered heteroaryl group comprising heteroatom taken among O, N and S; or it (X₅) represents -COOX₁₀ wherein X₁₀ represents (C₁-C₈)-alkyl or (C₂-C₈)-alkenyl; R_7a represents (C₁-C₂₀)-alkyl or (C₂-C₂₀)-alkenyl; Ac represents acetyl group. These compounds possess an anti-tumor activity. Also, invention relates to a method for inhibition of tumor growth in mammals and to a pharmaceutical composition based on synthesized compounds. Invention provides preparing new derivatives of taxanes possessing the enhanced anti-tumor activity and reduced toxicity as compared with taxol and taxoter.

EFFECT: improved and valuable medicinal properties of compounds.

39 cl, 4 tbl, 10 ex