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公开(公告)号：KR100321844B1
公开(公告)日：2004-05-24
申请号：KR1019980057837
申请日：1998-12-23
Applicant: 한국화학연구원
IPC: C07H17/00
Abstract: 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.
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2.发明公开4'-오-데메틸-에피포도필로톡신-베타-디-글루코시드의새로운아세탈유도체,이의제조방법및이를포함하는항암제조성물 失效新型缩醛衍生物4'-o-demethyl-epi-grape pilotoxin-beta-di-glucoside及其制备方法和含有它们的抗癌组合物
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