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

. Ankit; R. Kumar; T. Wang; R.N. Veedu; S. Kumar

doi:10.1080/15257770.2022.2029883

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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

Journal article

Peer reviewed

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

. Ankit, R. Kumar, T. Wang, R.N. Veedu and S. Kumar

Nucleosides, Nucleotides & Nucleic Acids, pp.1-18

2022

DOI: https://doi.org/10.1080/15257770.2022.2029883

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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.

Details

Title: Novel 3′-[4-fluoroaryl-(1,2,3-triazol-1-yl)]-3′-deoxythymidine analogues: Design, synthesis, characterization and their potential as anticancer agents
Authors/Creators: . Ankit (Author/Creator)
R. Kumar (Author/Creator) - Deenbandhu Chhotu Ram University of Science and Technology
T. Wang (Author/Creator) - Murdoch University
R.N. Veedu (Author/Creator) - Murdoch University
S. Kumar (Author/Creator) - Kurukshetra University
Publication Details: Nucleosides, Nucleotides & Nucleic Acids, pp.1-18
Publisher: Taylor & Francis
Identifiers: 991005545237307891
Murdoch Affiliation: Centre for Molecular Medicine and Innovative Therapeutics
Language: English
Resource Type: Journal article

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Collaboration types: Domestic collaboration; International collaboration
Citation topics: 2 Chemistry; 2.1 Synthesis; 2.1.1402 Click Chemistry
Web Of Science research areas: Biochemistry & Molecular Biology
ESI research areas: Biology & Biochemistry