申请人:WISCONSIN ALUMNI RESEARCH FOUNDATION
公开号:EP0426467A1
公开(公告)日:1991-05-08
Prodrugs for the treatment of kidney tumors are disclosed. The prodrugs are conjugates that can require the cooperation of multiple enzymes in the kidney to release 6-mercaptopurine or 6-thioguanine, or can selectively release 6-thioguanine. The prodrugs have the formula:
wherein R₁ is H or NH₂, x is 1 or 2 and R₂ represents various carboxylic acid or ester groupings, generally containing an animo and/or amido group.
本研究公开了用于治疗肾脏肿瘤的原药。这些原药是共轭物,可以需要肾脏中多种酶的合作来释放 6-巯基嘌呤或 6-硫鸟嘌呤,或者可以选择性地释放 6-硫鸟嘌呤。这些原药的结构式如下
其中,R₁ 是 H 或 NH₂,x 是 1 或 2,R₂ 代表各种羧酸或酯基,通常含有阿米诺和/或氨基。