ACETAL DERIVATIVES OF 4'-O-DEMETHYL-EPIPODOPHYLLOTOXIN-a-D-GLUCOSIDE, PREPARATION METHOD THEREOF AND ANTICANCER COMPOSITION CONTAINING THE SAME

摘要

PURPOSE: Acetal derivatives of 4'-O-demethyl-epipodophyllotoxin-a-D-glucoside, a preparation method thereof and an anticancer composition containing the same derivatives are provided, which compounds inhibit activity of human DNA topoisomerase II, and have improved or similar inhibiting activity on the growth of a cancer cell to a prior anticancer compound etoposide, so that it can be useful for prevention and treatment of cancer. CONSTITUTION: The acetal derivatives of 4'-O-demethyl-epipodophyllotoxin-a-D-glucoside represented by formula (1) are provided, wherein R1 and R2 are independently hydrogen, or C2-C12 alkenyl optionally substituted with one or more radicals selected from alkoxy, phenyl, substituted phenyl, halogen, nitro, cyano, hydroxy, carboxyl and amino, C2-C12 alkynyl, C2-C12 alkoxyalkyl or cyclopropyl, or form C5-C15 ring optionally substituted with one or more radicals selected from alkoxy, phenyl, substituted phenyl, halogen, nitro, cyano, hydroxy, carboxyl and amino, provided that R1 and R2 are not hydrogen simultaneously. The method for preparing the acetal derivatives of 4'-O-demethyl-epipodophyllotoxin-a-D-glucoside of formula (I) comprises reacting 4'-O-demethyl-epipodophyllotoxin-a-D-glucoside of formula (II) with aldehyde compound of formula (III) or acetal compounds of formula (IV) under acid catalyst, wherein R3 is C1-3 alkyl.