Benzocyclodecane derivatives with antitumor activity

摘要

A compound which is a benzocyclodecane of the formula I: wherein: at positions 8-9 and 11-12 independently represents a single or double bond, -R₁ is -O, or -OR₇, R₇ is H, C₁-C₇ alkanoyl, benzoyl, C₁-C₁₀ alkyl, C₂-C₁₀ alkenyl or COCH-CHR₈, R₈ is aryl or heterocyclyl; -R₂ and -R₃ are H, -O or -OR₉, R₉ is H, C₁-C₇ alkanoyl or benzoyl; when at position 11-12 there is a single bond, then -R₄ represents -O, -CH₂, -CHCOOR₁₀, R₁₀ is C₁-C₁₀ alkyl or aryl; -CH(OCH₃), -OR₉; -CH₂OR₁₁, R₁₁ is H or a sugar residue, -COR₁₂, R₁₂ is H, -OH or -OR₁₀; or when at position 11-12 there is a double bond, then -R₄ is -CH₂OR₁₁ or -COR₁₂; -R₅ and -R₆ are H or, when at position 8-9 there is a single bond, taken together form a cyclopropane ring; R₁₃ is H or 1-3 substituents selected from C₁-C₆ alkyl, C₂-C₆ alkenyl, phenyl, phenyl C₁-C₆ alkyl, halogen, hydroxy, C₁-C₆ alkoxy, aryloxy, cyano, nitro, amino, C₁-C₁₀ alkylamino, arylamino, C₁-C₇ alkanoylamino, aroylamino, hydroxycarbonyl, aminocarbonyl, C₁-C₆ alkylcarbonyl, C₁-C₆ alkylaminosulfonyl and arylaminosulfonyl group; with the provisos that if R₁ and R₄ -O, then one of R₂, R₃, R₅, R₆ and R₁₃ is not H atom; or a pharmaceutically acceptable salt thereof. These benzocyclodecane derivatives are endowed with antitumor activity; a process and new intermediates for their preparation, the pharmaceutical compositions containing them, and their use in the prevention, control and treatment of cancer are also provided.