申请人:Kuraray Co., Ltd.
公开号:US05032680A1
公开(公告)日:1991-07-16
2'-Deoxy-5-fluorouridine derivatives of the formula ##STR1## wherein, R.sup.1 is hydrogen atom or an acyl group and R.sup.2 and R.sup.3 are respectively hydrogen atom, an acyl group or a group of the formula ##STR2## wherein X.sup.1 and X.sup.2 are respectively oxygen atom or sulfur atom; R.sup.4 is a phenyl group, a benzyl group or a naphthyl group each of which may be substituted by an alkyl group, an alkoxyl group, an alkoxycarbonyl group, an alkylthio group, and acyl group, a halogen atom, trifluoromethyl group, nitro group, cyano group, carboxyl group and/or methylenedioxy group and R.sup.5 is an alkyl group, an alkenyl group or one of the groups represented by R.sup.4 which is the same as or different from R.sup.4, at least one of R.sup.2 and R.sup.3 being a group of the formula ##STR3## which exhibit excellent antitumour activities and have lower toxicity, methods of the production thereof and antitumour compositions containing said 2'-deoxy-5-fluorouridine derivatives.
2'-脱氧-5-氟尿苷衍生物的化学式为##STR1##其中,R.sup.1是氢原子或酰基,R.sup.2和R.sup.3分别是氢原子,酰基或化学式##STR2##中的基团,其中X.sup.1和X.sup.2分别是氧原子或硫原子;R.sup.4是苯基,苄基或萘基,每个基团都可以被烷基,烷氧基,烷氧羰基,烷硫基,酰基,卤素原子,三氟甲基基团,硝基,氰基,羧基和/或亚甲氧基取代,R.sup.5是烷基,烯基或由R.sup.4表示的基团之一,与R.sup.4相同或不同,R.sup.2和R.sup.3中至少有一个是化学式##STR3##的基团,这些衍生物表现出优异的抗肿瘤活性,毒性较低,制备方法和含有所述2'-脱氧-5-氟尿苷衍生物的抗肿瘤组合物。