Novel 3′-[4-fluoroaryl-(1,2,3-triazol-1-yl)]-3′-deoxythymidine analogues: Design, synthesis, characterization and their potential as anticancer agents

Ankit, ., Kumar, R., Wang, T., Veedu, R.N. and Kumar, S. (2022) 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 . pp. 1-18.

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.

Item Type:	Journal Article
Murdoch Affiliation(s):	Centre for Molecular Medicine and Innovative Therapeutics (CMMIT)
Publisher:	Taylor & Francis
URI:	http://researchrepository.murdoch.edu.au/id/eprint/63882

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