New azolyl-derivatives as multitargeting agents against breast cancer and fungal infections: synthesis, biological evaluation and docking study.
Antifungal Agents
/ chemical synthesis
Antineoplastic Agents
/ chemical synthesis
Aromatase Inhibitors
/ chemical synthesis
Azo Compounds
/ chemical synthesis
Breast Neoplasms
/ drug therapy
Candida
/ drug effects
Cell Proliferation
/ drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Female
Humans
MCF-7 Cells
Molecular Docking Simulation
Molecular Structure
Mycoses
/ drug therapy
Structure-Activity Relationship
Aromatase
breast cancer
Journal
Journal of enzyme inhibition and medicinal chemistry
ISSN: 1475-6374
Titre abrégé: J Enzyme Inhib Med Chem
Pays: England
ID NLM: 101150203
Informations de publication
Date de publication:
Dec 2021
Dec 2021
Historique:
entrez:
22
7
2021
pubmed:
23
7
2021
medline:
2
9
2021
Statut:
ppublish
Résumé
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
Identifiants
pubmed: 34289751
doi: 10.1080/14756366.2021.1954918
pmc: PMC8300937
doi:
Substances chimiques
Antifungal Agents
0
Antineoplastic Agents
0
Aromatase Inhibitors
0
Azo Compounds
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
1632-1645Références
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