ISSN print edition: 0366-6352 ISSN electronic edition: 1336-9075 Registr. No.: MK SR 9/7 Published monthly

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

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

Department of Chemistry, Pontifical Catholic University of Rio de Janeiro (PUC-Rio), Rio de Janeiro, Brazil

E-mail: ivan.iurchenko@umanitoba.ca

Received: 7 April 2026  Accepted: 8 June 2026

Abstract:

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

Keywords: Indolizine derivatives; Heterocyclic synthesis; 2-bromo-1-(2-oxo-2-phenylethyl)pyridin-1-ium bromide; Arylamide derivatives; Anticancer activity; Antiviral activity

Full paper is available at www.springerlink.com.

DOI: 10.1007/s11696-026-05188-4

Chemical Papers 80 (11) 13407–13420 (2026)