摘要
2,4-二氨基-6-[N-甲基(对氯苄基)氨基]喹唑啉盐酸盐(SIPI-759)属非经典叶酸拮抗剂。体外抑制 L 1210白血病细胞株,IC_(50)值为9.46×10^(-5)μg/ml;能明显损害 HeLa S3细胞形态;对 HeLa S3的集落形成在0.05 μg/ml 时抑制率达90％以上。体内生命延长率对 EAC 达250%;对 L615为131%;对足趾接种的 Lewis 肺癌抑瘤率为50～70%。本品以前体参入法对 L1210、L5178y DNA 及 RNA 均有抑制作用;对二氢叶酸还原酶的作用与 MTX 接近,但 L1210 MTX 耐药株对本品具交叉耐药性。
2,4-Diamino-6-[N-methyl(4-chlorobenzyl)amino]quinazoline(SIPI-759)is a non-classic antagonist of folic acid.Its IC_(50) value in culturedL1210 cells was 9.46×10^(-5)μg/ml.The morphological damage of HeLa S3 cellswas apparent and dose-dependent.The inhibition rate of colony formation ofHeLa S3 cells was above 90% at a dose of 0.05 μg/ml.In vivo,the transplantedtumors such as Ehrlich ascites carcinoma,L615,Lewis and B16 as well as humanlung carcinoma xenograft(LAX)were treated and showed different response toSIPI-759.The mechanism of antitumor activity of SIPI-759 was also studied.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
1991年第1期14-17,共4页
Chinese Journal of Pharmaceuticals
基金
新药研究基金
关键词
SIPI759
抗癌药
SIPI-759
antitumor
in vitro
in vivo
mechanism
