期刊
MOLECULAR DIVERSITY
卷 25, 期 1, 页码 307-321出版社
SPRINGER
DOI: 10.1007/s11030-020-10082-6
关键词
Alkoxy-coumarins; Auraptene; Umbelliprenin; Breast cancer
类别
资金
- State Scholarships Foundation (IKY): Grant Scheme for Postgraduate Studies in Secondary Education of the Operational Program Human Resource Development, Education and Lifelong Learning of the NSRF 2014-2020
- State Scholarships Foundation (IKY): European Social Fund
- EPSRC
Coumarin derivatives show inhibitory effects on human invasive breast ductal carcinoma cells, with compounds containing two prenyloxy groups or an octyloxy substituent showing higher potency. Breast cancer cells cultured under conditions that mimic the tumor microenvironment exhibit increased toxicity from potent compounds.
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. [GRAPHICS] .
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