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<p>A series of novel 2-amino-3-benzoyl-N-indolizine-1-carboxamide derivatives were synthesized in moderate to good yields (55–73%) via the reaction of 2-bromo-1-(2-oxo-2-phenylethyl)pyridin-1-ium bromide with 2-cyano-<i>N</i>-arylacetamides in dimethylformamide (DMF) in the presence of two molar equivalents of triethylamine (TEA). The structures of the synthesized compounds were confirmed by <sup>1</sup>H NMR, <sup>13</sup>C NMR, and LC–MS analyses. Five compounds, <b>5a, 5b, 5e, 5k,</b> and <b>5o</b>, were evaluated for anticancer activity against the NCI-60 panel of human cancer cell lines. Among the tested compounds, 2-amino-3-benzoyl-<i>N</i>-(2,3-dimethylphenyl)indolizine-1-carboxamide (<b>5e</b>) exhibited the most pronounced inhibitory profile, particularly against the non-small-cell lung cancer cell line HOP-62 and the renal cancer cell line ACHN. In addition, compounds <b>5i</b> and <b>5j</b> exhibited antiviral activity against influenza A H1N1 (California/07/2009) and H3N2 (Brisbane/10/2007) strains. These findings identify 2-amino-3-benzoylindolizine derivatives as promising scaffolds for further anticancer and antiviral optimization.</p> Graphical abstract <p></p>

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Design, synthesis, and in vitro anticancer and anti-influenza evaluation of 2-amino-3-benzoyl-N-indolizine-1-carboxamide derivatives

  • 期刊论文

  • 发表日期：

    2026年6月24日

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  • Anatolii Demchenko,
  • Ivan Iurchenko,
  • Volodymyr Zaitsev,
  • Yevhenii Novodvorskyi,
  • Volodymyr Sukhovieiev,
  • Lida Zavodovska,
  • Sergii Demchenko,
  • Sergii Tarnavsky,
  • Sergii Yarmoluk

摘要

A series of novel 2-amino-3-benzoyl-N-indolizine-1-carboxamide derivatives were synthesized in moderate to good yields (55–73%) via the reaction of 2-bromo-1-(2-oxo-2-phenylethyl)pyridin-1-ium bromide with 2-cyano-N-arylacetamides in dimethylformamide (DMF) in the presence of two molar equivalents of triethylamine (TEA). The structures of the synthesized compounds were confirmed by 1H NMR, 13C NMR, and LC–MS analyses. Five compounds, 5a, 5b, 5e, 5k, and 5o, were evaluated for anticancer activity against the NCI-60 panel of human cancer cell lines. Among the tested compounds, 2-amino-3-benzoyl-N-(2,3-dimethylphenyl)indolizine-1-carboxamide (5e) exhibited the most pronounced inhibitory profile, particularly against the non-small-cell lung cancer cell line HOP-62 and the renal cancer cell line ACHN. In addition, compounds 5i and 5j exhibited antiviral activity against influenza A H1N1 (California/07/2009) and H3N2 (Brisbane/10/2007) strains. These findings identify 2-amino-3-benzoylindolizine derivatives as promising scaffolds for further anticancer and antiviral optimization.

Graphical abstract