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, CO2¿CH¿3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C1-C18 alkoxy, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, 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.