申请人:SANKYO COMPANY LIMITED
公开号:EP0350315A1
公开(公告)日:1990-01-10
Rhizoxin and rhizoxin-2-ene derivatives of formula (I):
[in which: n is 1 to 25; A is an extra bond or oxygen, X is oxygen, sulphur, nitrogen or carbonyl; and R is hydrogen, carboxylic acyl having from 1 to 25 carbon atoms, alkoxycarbonyl group having from 2 to 26 carbon atoms, phosphono, alkylphosphono group in which the alkyl part has from 1 to 25 carbon atoms, dialkylphosphono group in which each alkyl part has from 1 to 25 carbon atoms, alkyl group having from 1 to 25 carbon atoms, aralkyl, cycloalkyl, heterocyclic, alkylthio group in which the alkyl part has from 1 to 25 carbon atoms, aralkylthio, or heterocyclylthio, or when X represents a nitrogen atom, R is R¹ and R², where R¹ and R² are hydrogen, alkyl, acyl, alkoxycarbonyl, phosphono, alkylphosphono or dialkylphosphono] have valuable anti-tumour activity. They may be prepared by acylation of rhizoxin or rhizoxin-2-ene.
式(I)的根肿灵和根肿灵-2-烯衍生物:
其中n 为 1 至 25;A 为额外键或氧,X 为氧、硫、氮或羰基;和 R 是氢、具有 1 至 25 个碳原子的羧酰基、具有 2 至 26 个碳原子的烷氧羰基、膦酰基、烷基膦酰基(其中烷基部分具有 1 至 25 个碳原子)、二烷基膦酰基(其中每个烷基部分具有 1 至 25 个碳原子)、具有 1 至 25 个碳原子的烷基、或当 X 代表氮原子时,R 为 R¹ 和 R²,其中 R¹ 和 R²为氢、烷基、酰基、烷氧羰基、膦酰基、烷基膦酰基或二烷基膦酰基]具有重要的抗肿瘤活性。它们可通过 rhizoxin 或 rhizoxin-2-ene 的酰化反应制备。