Rok 2024

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

  Publikacja

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

  - Scientific Reports - Rok 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...

  Pełny tekst do pobrania w portalu

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

  Publikacja

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

  - EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY - Rok 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,...

  Pełny tekst do pobrania w portalu