Year 2024

• Meldrum’s acid assisted formation of tetrahydroquinolin‑2‑one derivatives a short synthetic pathway to the biologically useful scaffold

  Publication

  • M. Ryczkowska
  • A. Trocka
  • A. Hromova
  • S. Makowiec

  - Scientific Reports - Year 2024

  A new method for the preparation of tetrahydroquinolin-2-one derivatives is presented. This approach involves a two-step reaction between enaminones and acylating agents, immediately followed by electrophilic cyclization, all within a single synthesis procedure, eliminating the need to isolate intermediates. The entire process is facilitated by the use of acyl Meldrum’s acids which not only shortens the preparation time of the...

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• Synthesis and biological evaluation of novel 3,6- amide and thioamide substituted- 2,3,4,9-tetrahydro-1H-carbazoles for anti-cancer activity

  Publication

  • A. Trocka
  • A. Kallingal
  • N. Maciejewska
  • N. Magdalena
  • A. Hromova
  • S. Makowiec

  - EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY - Year 2024

  Herein, we report the synthesis of new compounds with demonstrated anticancer properties based on the 2,3,4,9- tetrahydro-1H-carbazole scaffold. The Fischer indolization method was used to close the heterocyclic motif. The synthesis method’s scope and limitations were thoroughly assessed through a series of experiments. Biological assays revealed that two thioamide compounds exhibited significant anticancer activity against MCF-7,...

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