Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 36, Issue 1, Pages 1632-1645Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2021.1954918
Keywords
Aromatase; breast cancer
Funding
- Italian Ministry for University and Research (MIUR) [FISR2019_04819 BacCAD]
- University G. d'Annunzio
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New indazole and triazole derivatives were synthesized and evaluated for their potential dual activities as agents targeting both aromatase and inducible nitric oxide synthase. Some compounds showed promising effects in treating breast cancer and also exhibited antifungal properties against Candida strains.
Nonsteroidal aromatase inhibitors (NSAIs) are well-established drugs for the therapy of breast cancer. However, they display some serious side effects, and their efficacy can be compromised by the development of chemoresistance. Previously, we have reported different indazole-based carbamates and piperidine-sulphonamides as potent aromatase inhibitors. Starting from the most promising compounds, here we have synthesised new indazole and triazole derivatives and evaluated their biological activity as potential dual agents, targeting both the aromatase and the inducible nitric oxide synthase, being this last dysregulated in breast cancer. Furthermore, selected compounds were evaluated as antiproliferative and cytotoxic agents in the MCF-7 cell line. Moreover, considering the therapeutic diversity of azole-based compounds, all the synthesized compounds were also evaluated as antifungals on different Candida strains. A docking study, as well as molecular dynamics simulation, were carried out to shed light on the binding mode of the most interesting compound into the different target enzymes catalytic sites.
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