Abstract
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.Graphic abstract
Highlights
Breast carcinoma is considered the predominant and more common malignancy in women worldwide, with one in eight women potentially developing breast cancer during their lifetime [1] and predictions of 3.2 million newly diagnosed cases per year by 2050 [2]
The new series were designed in order to evaluate the influence of the disubstitution as well as the length of the lipophilic chain in the cytotoxicity against breast cancer cell lines
The results of this study indicate that alkylation modification induces noticeable differentiation in pharmacological activity of coumarins
Summary
Breast carcinoma is considered the predominant and more common malignancy in women worldwide, with one in eight women potentially developing breast cancer during their lifetime [1] and predictions of 3.2 million newly diagnosed cases per year by 2050 [2]. While many biological and physicochemical factors have been identified in cancer development, there is an increasing interest in the role of inflammation and involvement of stromal component of the tumour microenvironment [3]. The challenge of treating breast cancer resides in the identification of active compounds capable of targeting the cancer, but mainly in identifying potent therapies with low side effects [4]. In this perspective, natural compounds like coumarins have gained significant interest in the recent years for their numerous pharmacological activities including chemopreventive and antiproliferative properties against various cancer types [5,6,7,8]. Natural and synthetic coumarins have been reported as effective chemopreventive and anticancer agents in vitro [23,24,25,26] and in vivo [27]
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