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SYNTHESIS AND ANTITUMOR-ACTIVITY OF PT(II) COMPLEXES OF ESTRADIOL DERIVATIVES

被引：9
作者：
BRUNNER, H
SPERL, G
机构：
来源：
MONATSHEFTE FUR CHEMIE | 1993年 / 124卷 / 01期
关键词：
ESTRADIOL DERIVATIVES; PLATINUM(II) COMPLEXES; HUMAN MAMMARY CARCINOMA CELL LINES MDA-MB 231 AND MCF-7; ANTITUMOR ACTIVITY; ESTROGEN-RECEPTOR BINDING;
D O I：
10.1007/BF00808513
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
Estrogen-receptor binding moieties were introduced into Pt(II) complexes in order to facilitate the selective transport into cancer cells. Estradiol esters of 2,3-diaminopropionic acid and estradiol ethers of 1,2-diamino-2-methyl-3-(p-hydroxyphenyl)propane were attached to Pt(II) complexes. The antitumor activity of the compounds was tested towards the human mammary carcinoma cell lines MDA-MB 231 and MCF-7, respectively, and the estrogen-receptor binding affinity of the Pt(II) complexes was determined. The steroidal Pt(II) complexes gave a maximum growth inhibition of 80% and a maximum estrogen-receptor binding affinity of 5.18.
引用
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页码：83 / 102
页数：20
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