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dc.contributor.authorCarradori, Simone
dc.contributor.authorMaccallini, Cristina
dc.contributor.authorAmoroso, Rosa
dc.contributor.authorCataldi, Amelia
dc.contributor.authorFantacuzzi, Marialuigia
dc.contributor.authorGiampietro, Letizia
dc.contributor.authorDe Filippis, Barbara
dc.contributor.authorAmmazzalorso, Alessandra
dc.contributor.authorAKDEMİR, ATİLLA
dc.contributor.authorSisto, Francesca
dc.contributor.authorGallorini, Marialucia
dc.date.accessioned2021-08-03T20:59:25Z
dc.date.available2021-08-03T20:59:25Z
dc.date.issued2021-01-01T00:00:00Z
dc.identifier.urihttp://hdl.handle.net/20.500.12645/29117
dc.description.abstractNonsteroidal 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.
dc.subjectMaccallini C., Gallorini M., Sisto F., AKDEMİR A., Ammazzalorso A., De Filippis B., Fantacuzzi M., Giampietro L., Carradori S., Cataldi A., et al., -New azolyl-derivatives as multitargeting agents against breast cancer and fungal infections: synthesis, biological evaluation and docking study-, JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.36, sa.1, ss.1632-1645, 2021
dc.titleNew azolyl-derivatives as multitargeting agents against breast cancer and fungal infections: synthesis, biological evaluation and docking study
dc.typeArticle
dc.identifier.wosWOS:000675630300001
dc.identifier.doi10.1080/14756366.2021.1954918
dc.identifier.pubmed34289751
local.publication.isinternational1


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