Quinoline-imidazole/benzimidazole derivatives as dual-/multi-targeting hybrids inhibitors with anticancer and antimicrobial activity.
14-alpha Demethylase Inhibitors
/ pharmacology
Anti-Bacterial Agents
/ pharmacology
Antifungal Agents
/ pharmacology
Antineoplastic Agents
/ pharmacology
Benzimidazoles
/ pharmacology
Breast Neoplasms
Cell Line, Tumor
Dermatologic Agents
/ pharmacology
Drug Screening Assays, Antitumor
Escherichia coli
Female
Gentamicins
Humans
Imidazoles
Leukemia
Molecular Structure
Quinolines
/ pharmacology
Salts
Staphylococcus aureus
Structure-Activity Relationship
Journal
Scientific reports
ISSN: 2045-2322
Titre abrégé: Sci Rep
Pays: England
ID NLM: 101563288
Informations de publication
Date de publication:
10 10 2022
10 10 2022
Historique:
received:
05
05
2022
accepted:
27
09
2022
entrez:
10
10
2022
pubmed:
11
10
2022
medline:
13
10
2022
Statut:
epublish
Résumé
Two new classes of hybrid quinoline-imidazole/benzimidazole derivatives (the hybrid QIBS salts and QIBC cycloadducts) were designed and synthesized to evaluate their anticancer and antimicrobial activity. The strategy adopted for synthesis is straight and efficient, in four steps: N-acylation, N-alkylation, quaternization and a Huisgen 3 + 2 cycloaddition. The in vitro single-dose anticancer assay of forty six hybrid quinoline-benzimidazole compounds reveal that one QIBS salt (11h), has an excellent quasi nonselective activity against all type of cancer cell with an excellent PGI in the area of 90-100% and very good lethality. Three others quinoline-imidazole/benzimidazole hybrids (8h, 12h, 12f) has an excellent selective activity against some cancer cell lines: breast cancer MDA-MB-468 and Leukemia HL-60 TB). The five-dose assay screening confirms that compound 11h possesses excellent anti-proliferative activity, with GI
Identifiants
pubmed: 36216981
doi: 10.1038/s41598-022-21435-6
pii: 10.1038/s41598-022-21435-6
pmc: PMC9551061
doi:
Substances chimiques
14-alpha Demethylase Inhibitors
0
Anti-Bacterial Agents
0
Antifungal Agents
0
Antineoplastic Agents
0
Benzimidazoles
0
Dermatologic Agents
0
Gentamicins
0
Imidazoles
0
Quinolines
0
Salts
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
16988Informations de copyright
© 2022. The Author(s).
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