Antitumoral compounds

摘要

New spisulosine derivatives of use in treating tumors are of the formula (I) wherein: each X is the same or different, and represents H, OH, OR', SH, SR', SOR', SO₂R', NO₂, NH₂, NHR', N(R')₂, CN, halogen, C(-O)H, C(-O)CH₃, CO₂H, CO₂CH₃, substituted or unsubstituted C₁-C₁₈ alkyl, substituted or unsubstituted C₂-C₁₈ alkenyl, substituted or unsubstituted C₂-C₁₈ alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, or two groups X may together form -O; Y is NR₁, OR₁, PR₁, SR₁, or halogen, wherein the number of substituents R₁ is selected to suit the valency and each R₁ is independently selected of H, OH, C(-O)R', P(-O)R'R'', substituted or unsubstituted C₁-C₁₈ alkyl, substituted or unsubstituted C₂-C₁₈ alkenyl, substituted or unsubstituted C₂-C₁₈ alkynyl, substituted or unsubstituted aryl, and wherein the dotted line indicates an optional double bond; each Z is the same different, and represents H, OH, OR', SH, SR', SOR', SO₂R', NO₂, NH₂, NHR', N(R')₂, NHC(O)R', CN, halogen, C(-O)H, C(-O)CH₃, CO₂H, CO₂CH₃, substituted or unsubstituted C₁-C₁₈ alkyl, substituted or unsubstituted C₂-C₁₈ alkenyl, substituted or unsubstituted C₂-C₁₈ alkenyl, substituted or unsubstituted C₂-C₁₈ alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, or two groups Z may together form -O; z is 0 to 25; y is to 0 to 20; R₂ is H, C(-O)R', P(-O)R'R'', S(-O)R'R'', S(-O)₂R', substituted or unsubstituted C₁-C₁₈ alkyl, substituted or unsubstituted C₂-C₁₈ Alkenyl, substituted or unsubstituted C₂-C₁₈ alkynyl, substituted or unsubstituted aryl; R₃ is H, C(-O)R', P(-O)R'R'', S(-O)R'R'', S(-O)₂R', substituted or unsubstituted C₁-C₁₈ alkyl, substituted or unsubstituted C₂-C₁₈ alkenyl, substituted or unsubstituted C₂-C₁₈ alkynyl, substituted or unsubstituted aryl; each of the R', R'' groups is independently selected from the group consisting of H, OH, NO₂, NH₂, SH, CN, halogen, -O, C(-O)H, C(-O)CH₃, CO₂H, CO_2CH3, substituted or unsubstituted C₁-C₁₈ alkyl, substituted or unsubstituted C₁-C₁₈ alkoxy, substituted or unsubstituted C₂-C₁₈ alkenyl, substituted or unsubstituted C₂-C₁₈ alkynl, substituted or unsubstituted aryl; there may be one or more unsaturations in the hydrocarbon backbone defined by the chain (II) and salts thereof; with the exception of a C₁₆-C₂₄ 2-amino-3-hydroxyalkane or a C₁₆-C₂₄ 2-amino-3-hydroxyalkene