AN ESTRADIOL-LINKED NITROSOUREA AND SITE-DIRECTED CHEMOTHERAPY IN MAMMARY-CARCINOMA

被引：5

作者：

BETSCH, B ^{[1
]}

BERGER, MR ^{[1
]}

SPIEGELHALDER, B ^{[1
]}

SCHMAHL, D ^{[1
]}

EISENBRAND, G ^{[1
]}

机构：

[1] UNIV KAISERSLAUTERN,DEPT FOOD CHEM & ENVIRONM TOXICOL,W-6750 KAISERSLAUTERN,GERMANY

来源：

EUROPEAN JOURNAL OF CANCER | 1990年 / 26卷 / 08期

关键词：

D O I：

10.1016/0277-5379(90)90194-X

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

The half-life, peak concentration, peak accumulation and tissue availability of the DNA-crosslinking nitrosourea 1-(2-chloroethyl)-1-nitrosocarbamoyl-L-alanine (CNC-alanine) and its oestradiol-linked derivative (CNC-alanine-oestradiol-17-ester) were studied in liver, lung, spleen, uterus and mammary carcinomas in female Sprague-Dawley rats with chemically induced mammary carcinomas. Compared with CNC-alanine, the ester had a longer half-life, higher peak concentration, increased peak accumulation and enhanced tissue availability in all tissues. In oestradiol receptor positive mammary carcinomas, the oestradiol-linked drug showed a 2 times higher peak concentration, a 5 times longer half-life, a 10 times increased peak accumulation and a 20 times greater tissue availability compared with CNC-alanine. Oestradiol-linked nitrosoureas may offer new perspectives for site-directed chemotherapy of oestradiol receptor positive breast cancer. © 1990.

引用

页码：895 / 898

页数：4

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