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Novel 3′-[4-fluoroaryl-(1,2,3-triazol-1-yl)]-3′-deoxythymidine analogues: Design, synthesis, characterization and their potential as anticancer agents.
- Source :
- Nucleosides, Nucleotides & Nucleic Acids; 2022, Vol. 41 Issue 4, p343-360, 18p
- Publication Year :
- 2022
-
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 <superscript>1</superscript>H NMR, <superscript>13</superscript>C 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 IC<subscript>50</subscript> 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. [ABSTRACT FROM AUTHOR]
- Subjects :
- ANTINEOPLASTIC agents
LIVER cells
LIVER cancer
CANCER cells
NUCLEOSIDES
Subjects
Details
- Language :
- English
- ISSN :
- 15257770
- Volume :
- 41
- Issue :
- 4
- Database :
- Complementary Index
- Journal :
- Nucleosides, Nucleotides & Nucleic Acids
- Publication Type :
- Academic Journal
- Accession number :
- 157638839
- Full Text :
- https://doi.org/10.1080/15257770.2022.2029883