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首页> 外文期刊>British Journal of Cancer >3-Bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate inhibits cancer cell invasion in vitro and tumour growth in vivo
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3-Bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate inhibits cancer cell invasion in vitro and tumour growth in vivo

机译：3-溴苯基6-乙酰氧基甲基-2-氧代-2H-1-苯并吡喃-3-羧酸盐在体外抑制癌细胞侵袭和体内肿瘤生长

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摘要

In search for new anticancer agents, we have evaluated the antiinvasive and antimigrative properties of recently developed synthetic coumarin derivatives among which two compounds revealed important activity: 3-chlorophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate and 3-bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate. Both drugs were able to inhibit cell invasion markedly in a Boyden chamber assay, the bromo derivative being more potent than the reference matrix metalloprotease (MMP) inhibitor GI 129471. In vivo, tumour growth was reduced when nude mice grafted with HT1080 or MDA-MB231 cells were treated i.p. 3 days week?1 with the bromo coumarin derivative. These effects were not associated with the inhibition of urokinase, plasmin, MMP-2 or MMP-9. The mechanism of action of the drugs remains to be elucidated. However, these two coumarin derivatives may serve as new lead compounds of an original class of antitumour agents.
机译：为了寻找新的抗癌药，我们评估了最近开发的合成香豆素衍生物的抗侵袭和抗迁移特性，其中两种化合物显示出重要的活性：3-氯苯基6-乙酰氧基甲基-2-氧代-2H-1-苯并吡喃-3-羧酸酯和3-溴苯基6-乙酰氧基甲基-2-氧代-2H-1-苯并吡喃-3-羧酸酯。两种药物在Boyden室测定中均能显着抑制细胞侵袭，溴衍生物比参考基质金属蛋白酶（MMP）抑制剂GI 129471更有效。在体内，移植HT1080或MDA-MB231的裸鼠体内肿瘤生长会减少ip处理细胞每周3天？含溴香豆素衍生物。这些作用与抑制尿激酶，纤溶酶，MMP-2或MMP-9无关。药物的作用机理还有待阐明。然而，这两种香豆素衍生物可以用作抗肿瘤剂原始类别的新的先导化合物。

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