Coumarins possess a wide array of therapeutic capabilities, but often with unclear mechanism of action. We tested a small library of 18 coumarin derivatives against human invasive breast ductal carcinoma cells with the capacity of each compound to inhibit cell proliferation scored, and the most potent coumarin analogues selected for further studies. Interestingly, the presence of two prenyloxy groups (5,7-diprenyloxy-4-methyl-coumarin, 4g) or the presence of octyloxy substituent (coumarin 4d) was found to increase the potency of compounds in breast cancer cells, but not against healthy human fibroblasts. The activity of potent compounds on breast cancer cells cultured more similarly to the conditions of the tumour microenvironment was also investigated, and increased toxicity was observed. Results suggest that tested coumarin derivatives could potentially reduce the growth of tumour mass. Moreover, their use as (combination) therapy in cancer treatment might have the potential of causing limited side effects.

中文翻译：

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研究仿生香豆素类似物对人乳腺癌细胞的细胞毒性。

香豆素具有广泛的治疗能力，但通常作用机制不明确。我们测试了针对人类浸润性乳腺导管癌细胞的 18 种香豆素衍生物的小型文库，并对每种化合物抑制细胞增殖的能力进行了评分，并选择了最有效的香豆素类似物进行进一步研究。有趣的是，发现两个异戊二烯氧基（5,7-二异戊二烯氧基-4-甲基-香豆素，4g）或辛氧基取代基（香豆素 4d）的存在会增加化合物在乳腺癌细胞中的效力，但不会对健康人成纤维细胞。还研究了有效化合物对与肿瘤微环境条件更相似的乳腺癌细胞的活性，并观察到毒性增加。结果表明，经过测试的香豆素衍生物可能会减少肿瘤块的生长。此外，它们在癌症治疗中用作（组合）疗法可能会引起有限的副作用。