ACYLATED DERIVATIVE OF HOMOHARRINGTONINE, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF

摘要

The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and relates to novel homoharringtonine acylated derivatives of formula (I) and formula (II) and a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.;

主权项

1. An acylated homoharringtonine derivative of formula (I) or formula (II), wherein R1 and R2 are independently selected from H, C1-C20 alkyl, C2-C20 alkenyl, C4-C20 conjugated alkenyl, C3-C7 cycloalkyl or cycloalkenyl, aryl, heterocyclic radicals, heteroaryl, and amino acid side chain residues, which, except for H, are optionally substituted with one or more substituents selected from the group consisting of halogen, amino, C1-C6 alkyl amino, nitro, cyano, hydroxyl, C1-C6 alkoxy, thiol and C1-C6 alkylthio; said C3-C7 cycloalkyl or cycloalkenyl, aryl, heterocyclic radicals or heteroaryl are optionally substituted with C1-C6 alkyl; and said C1-C20 alkyl, C2-C20 alkenyl or C4-C20 conjugated alkenyl are optionally substituted with aryl or heteroaryl; or a pharmaceutically acceptable salt thereof.