DIORGANOTIN 2-FLUOROCINNAMATES AND 4-FLUOROPHENYLACETATES - SYNTHESIS, CHARACTERIZATION AND INVITRO ANTITUMOR-ACTIVITY

被引:77
作者
GIELEN, M
ELKHLOUFI, A
BIESEMANS, M
KAYSER, F
WILLEM, R
机构
[1] Free University of Brussels (VUB), Department of General and Organic Chemistry (AOSC), Brussels, B-1050
[2] Free University of Brussels (VUB), High Resolution NMR Centre
关键词
ORGANOTIN; ANTITUMOR; FLUOROCINNAMATE; FLUOROPHENYLACETATE;
D O I
10.1002/aoc.590070307
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
The synthesis and characterization by spectroscopy of several new di-n-butyltin and diethyltin 2-fluorocinnamates and 4-fluorophenylacetates are described. In vitro tests on two human tumour cell lines, MCF-7, a mammary tumour, and WiDr, a colon carcinoma, showed that two of these compounds are more active than cisplatin. Other in vitro tests performed by the NCI, USA on a panel of human tumour cell lines show that one of them, bis[di-n-butyl(2-fluorophenylacetato)tin] oxide, is characterized by statistically significant D(GI50), D(TGI) and D(LC50) sensitivities, but non-significant D(H) and MGD(H) selectivities, whereas the analogous 2-fluorocinnamate shows no such significant values.
引用
收藏
页码:201 / 206
页数:6
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