Novel 3'-[4-fluoroaryl-(1,2,3-triazol-1-yl)]-3'-deoxythymidine analogues: Design, synthesis, characterization and their potential as anticancer agents.
Nucleosides Nucleotides Nucleic Acids
; 41(4): 343-360, 2022.
Article
em En
| MEDLINE
| ID: mdl-35094645
ABSTRACT
Novel 3'-[4-fluoroaryl-(1,2,3-triazol-1-yl)]-3'-deoxythymidine analogues (7a-l) were developed by the Cu alkyne-azide cycloaddition (CuAAC) reaction. The obtained lead compounds were confirmed by using 1H NMR, 13C NMR, 2 D NMR, HRMS and their anticancer activities were screened against Huh-7 liver cancer cells and U87MG human glioblastoma cells. Among the synthesized fluorinated 1,2,3-triazolyl nucleosides, three compounds (7i, 7a-b) demonstrated promising anti-proliferative against Huh-7 and U87MG cell lines. Significantly, compound 7i has displayed remarkable promising anticancer activity with IC50 value in the micromole range (22.41-24.92 µM) and (18.12-21.36 µM) against Huh-7 cancer cells and U87MG glioblastoma cells, respectively.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Timidina
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Triazóis
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Glioblastoma
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Antineoplásicos
Limite:
Humans
Idioma:
En
Revista:
Nucleosides Nucleotides Nucleic Acids
Ano de publicação:
2022
Tipo de documento:
Article