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PreprintCC BYChemRxiv

Antimicrobial and cytotoxic activity of 2-amino-4H-chromenes

  • Jackson B. A. Silva1,2
  • Yan R. Robles1,2
  • Ana L. O. Santos3,4
  • Júlia G. Teixeira3,4
  • Tábata R. Esperandim5,6
  • Letícia H. dos Reis5,6
  • Maria A. S. C. Chellegatti7,2
  • Niege A. J. C. Furtado7,2
  • Carlos H. G. Martins5,6
  • Denise C. Tavares3,4
  • Larissa G. Maciel8,9
  • Antônio E. M. Crotti1,2
1 more authors
  • Antonio Eduardo Crotti
9 affiliations
  1. 1Department of Chemistry, Faculty of Philosophy, Sciences, and Letters of Ribeirão Preto
  2. 2University of São Paulo
  3. 3Institute of Biomedical Sciences
  4. 4Federal University of Uberlândia
  5. 5Research Center in Exact and Technological Sciences
  6. 6University of Franca
  7. 7Faculty of Pharmaceutical Sciences of Ribeirão Preto
  8. 8Department of Fundamental Chemistry
  9. 9Federal University of Pernambuco
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Abstract

Although some 2-amino-4H-chromenes displayed moderate activity against S. mitis (1, 2, 4, 5, 6, 7, 9, and 10), S. salivarius (3 and 9), and L. paracasei (1 and 6), most of the compounds displayed weak activity against most of the bacteria involved in dental caries and were inactive against C. albicans and C. krusei. On the other hand, compounds 4 (IC50 < 2.47 µM, SI > 2564) and 8 (IC50 = 37.74 µM, SI > 154.80) displayed the highest anticancer activity against the MCF-7 and HeLa cell lines. Although compounds 4 and 5 displayed only moderate activity against U-251MG cells, their high SI values (>82.78 and >81.60, respectively) make them promising candidates for further investigation as antiproliferative agents. Molecular docking simulations help us to rationalize potential molecular targets for compounds 1-10 reported herein. All molecules were docked into four receptors/enzymes (β-tubulin, CDK4/6, ERα, and EGFR), and in two of them (EGFR and CDK4/6), compounds 8R and 5R ranked favorably within their respective docking protocols and displayed relevant interactions with N842 and L83 residues in their respective active sites. These findings are consistent with in vitro cytotoxic assays and highlight the potential of compounds 1-10 to guide the design of more potent and selective anticancer candidates.

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Cite

BibTeXRIS
BibTeX
@misc{silva2026antimicrobial,
  title = {{Antimicrobial and cytotoxic activity of 2-amino-4H-chromenes}},
  author = {Jackson B. A. Silva and Yan R. Robles and Ana L. O. Santos and Júlia G. Teixeira and Tábata R. Esperandim and Letícia H. dos Reis and Maria A. S. C. Chellegatti and Niege A. J. C. Furtado and Carlos H. G. Martins and Denise C. Tavares and Larissa G. Maciel and Antônio E. M. Crotti and Antonio Eduardo Crotti},
  howpublished = {ChemRxiv},
  year = {2026},
  month = sep,
  doi = {10.26434/chemrxiv.15008338/v1},
  url = {https://chemrxiv.org/doi/full/10.26434/chemrxiv.15008338/v1},
  note = {CC BY},
}
RIS
TY  - UNPB
TI  - Antimicrobial and cytotoxic activity of 2-amino-4H-chromenes
AU  - Jackson B. A. Silva
AU  - Yan R. Robles
AU  - Ana L. O. Santos
AU  - Júlia G. Teixeira
AU  - Tábata R. Esperandim
AU  - Letícia H. dos Reis
AU  - Maria A. S. C. Chellegatti
AU  - Niege A. J. C. Furtado
AU  - Carlos H. G. Martins
AU  - Denise C. Tavares
AU  - Larissa G. Maciel
AU  - Antônio E. M. Crotti
AU  - Antonio Eduardo Crotti
PY  - 2026
DA  - 2026/09/04
PB  - ChemRxiv
DO  - 10.26434/chemrxiv.15008338/v1
UR  - https://chemrxiv.org/doi/full/10.26434/chemrxiv.15008338/v1
AB  - Although some 2-amino-4H-chromenes displayed moderate activity against S. mitis (1, 2, 4, 5, 6, 7, 9, and 10), S. salivarius (3 and 9), and L. paracasei (1 and 6), most of the compounds displayed weak activity against most of the bacteria involved in dental caries and were inactive against C. albicans and C. krusei. On the other hand, compounds 4 (IC50 < 2.47 µM, SI > 2564) and 8 (IC50 = 37.74 µM, SI > 154.80) displayed the highest anticancer activity against the MCF-7 and HeLa cell lines. Although compounds 4 and 5 displayed only moderate activity against U-251MG cells, their high SI values (>82.78 and >81.60, respectively) make them promising candidates for further investigation as antiproliferative agents. Molecular docking simulations help us to rationalize potential molecular targets for compounds 1-10 reported herein. All molecules were docked into four receptors/enzymes (β-tubulin, CDK4/6, ERα, and EGFR), and in two of them (EGFR and CDK4/6), compounds 8R and 5R ranked favorably within their respective docking protocols and displayed relevant interactions with N842 and L83 residues in their respective active sites. These findings are consistent with in vitro cytotoxic assays and highlight the potential of compounds 1-10 to guide the design of more potent and selective anticancer candidates.
ER  -