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<p>Synthesis of aryl derivatives of 5-azaindole linked 1,2,3-triazoles were achieved by the reaction between aryl azide and aryl alkynes in the presence of CuSO<sub>4</sub>.5H<sub>2</sub>O and Na-ascorbate in t-BuOH/H<sub>2</sub>O at room temperature over 12&#xa0;h time period. These synthesized derivatives were evaluated for their anticancer activity against MCF-7 (breast cancer), A549 (lung cancer), Colo-205 (colon cancer) &amp; A2780 (ovarian cancer) cell lines by using MTT assay reduction method with Etoposide as standard drug. Among them, compound <b>17i</b> with 3,5-dinitro substituent on the aryl moiety showed most promising activity against four cell lines like MCF-7, A549, Colo-205 and A2780 with IC<sub>50</sub> values of 0.01 ± 0.0071&#xa0;µM; 0.06 ± 0.0083&#xa0;µM; 1.19 ± 0.6700&#xa0;µM, 1.71 ± 0.7400&#xa0;µM respectively. The molecular docking studies revealed that <b>17i</b> and <b>17d</b> are identified to be the better compounds with the evaluated targets TopoII, EGFR and VEGFR2 based on their binding affinities and molecular recognition patterns with reference inhibitors.</p>

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Design, synthesis, in-vitro and in-silico anticancer evaluation of aryl derivatives of 5-azaindole linked 1,2,3-triazoles

  • 期刊论文

  • 发表日期：

    2026年5月12日

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  • L. Narasimhasana Reddy,
  • Reddymasu Sreenivasulu,
  • Ravikumar Kapavarapu,
  • Chandrasekar Kuppan

摘要

Synthesis of aryl derivatives of 5-azaindole linked 1,2,3-triazoles were achieved by the reaction between aryl azide and aryl alkynes in the presence of CuSO4.5H2O and Na-ascorbate in t-BuOH/H2O at room temperature over 12 h time period. These synthesized derivatives were evaluated for their anticancer activity against MCF-7 (breast cancer), A549 (lung cancer), Colo-205 (colon cancer) & A2780 (ovarian cancer) cell lines by using MTT assay reduction method with Etoposide as standard drug. Among them, compound 17i with 3,5-dinitro substituent on the aryl moiety showed most promising activity against four cell lines like MCF-7, A549, Colo-205 and A2780 with IC50 values of 0.01 ± 0.0071 µM; 0.06 ± 0.0083 µM; 1.19 ± 0.6700 µM, 1.71 ± 0.7400 µM respectively. The molecular docking studies revealed that 17i and 17d are identified to be the better compounds with the evaluated targets TopoII, EGFR and VEGFR2 based on their binding affinities and molecular recognition patterns with reference inhibitors.