Pharmaceutical compositions comprising aryl-substituted acyclic enediyne compounds

摘要

A pharmaceutical compositions comprises a compound of formula (I): or a pharmaceutically acceptable salt thereof: wherein R₁═R₂ ═H; or R₁ and R₂ together form a moiety represented by the formula R₃ represents a substituted or unsubstituted alkyl having 4-30 carbon atoms, or a substituted or unsubstituted aryl group having 3-30 carbon atoms; and R₄ represents a substituted or unsubstituted aryl group having 3-30 carbon atoms; with the proviso that R₃ is not butyl, pentyl, tetrahydropyranyloxymethyl, tetrahydropyranyloxypropyl or phenyl when R₁═R₂═H and R₄ is o-cyanophenyl,; and with the proviso that R₃ is not butyl when R₁═R₂═H and R₄ is phenyl. ;The pharmaceutical composition may be used to treat a subject afflicted with a tumor/cancer by inhibiting topoisomerase I activities or blocking the S phase or G2/M phase of the tumor/cancer cells.