4.6 Article

Synthesis, characterization andin vitroanticancer activity of thiabendazole-derived 1,2,3-triazole derivatives

Journal

NEW JOURNAL OF CHEMISTRY
Volume 44, Issue 28, Pages 12099-12106

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c9nj05685h

Keywords

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Funding

  1. MAScIR
  2. Moroccan Foundation for Advanced Science, Innovation and Research
  3. MESRSFC
  4. CNRST, Morocco [1970/15]

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A series of thiabendazole-derived 1,2,3-triazole compounds were synthesized in good yieldsvia1,3-dipolar cycloaddition through click chemistry approach using different chain alkyl azides with 4-(1-(prop-2-yn-1-yl)benzimidazole-2-yl)thiazole in the presence of copper(i) catalyst. These compounds were characterized on the basis of FT-IR,H-1 NMR,C-13 NMR as well as mass spectrometry. The newly synthesized compounds were screened for theirin vitroantiproliferative activity against a panel of three human cancer cell lines (HT29, MDA-MB-231 and SKBR3). Compound4gexhibited significant activity against all the cell lines tested, with IC(50)values ranging from 1.28 and 7.72 mu g mL(-1), inducing caspases 3 and 7, which further confirms the contribution of apoptotic cell death in MCF-7 and MDA-MB-231 cells. This work further demonstrates the anticancer properties of4g, inducing apoptotic cell death, and the structure activity association is also discussed. This product could be a promising chemotherapeutic agent for cancer treatment.

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