Compounds of the saframycin-ecteinascidin series, uses, and synthesis thereof

摘要

Compounds of the saframycin-ecteinascidin series with cytotoxic properties having the following general formula, their uses and synthesis, are disclosed: wherein R₁ and R₄ is H, a C₁ to C₄ alkyl group, or an acyl group; wherein R₂ is an ether, ester, amide, or a phthalimide group; wherein R₃ is -O, OH, an ether group, an acyl group such as OC(O)Me, OC(O)Bn and OC(O)Et, or a sulfide group; wherein R₅ is H, halogen, OH, an ether group, an acyl group, or an amide group; wherein R₆ is -O, OH, OCH₃, CN, or an acyloxy group; wherein R₇, is -O, OH, halogen, an ether group, or an acyl group; wherein R₈ and R₉ are independently H, CH₃, OCH₃, OC₂H₅, CF₃, halogen such as Br and F, or R₈ and R₉ are joined together as a methylenedioxy group, or other five or six membered ring; wherein R₁₀ and R₁₁ are independently CH₃, OCH₃, OC₂H₅, SCH₃, or SC₂H₅; wherein R₁₂ is H, a C₁ to C₄ alkyl group, or an acyl group; and wherein the chiral center marked * has the R or the S configuration.