Discovery of Novel Fluorescent Azaindoles with Cytotoxic Action in A2780 Ovarian Carcinoma Cells

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Abstract

Azaindole scaffold is a privileged structure in medicinal chemistry and some derivatives have demonstrated to be potential anticancer drugs. Herein, a set of novel azaindoles, comprising the four regioisomers, bearing a morpholine (azaindoles 3a-d) and N-methyl-N-benzylamine (azaindoles 4a-d) groups were prepared. Among these compounds, azaindoles 4 exhibited higher cytotoxicity against the ovarian cancer cell line A2780 and normal dermal fibroblasts compared to azaindoles 3. Furthermore, azaindoles 4b and 4c promoted a delay in the cell cycle of the cancer cell line, inspiring an investigation into the intracellular localization of these derivatives.
Original languageEnglish
Article numbere202400225
Number of pages7
JournalChemmedchem
Volume19
Issue number20
Early online date16 Jun 2024
DOIs
Publication statusPublished - 16 Oct 2024

Keywords

  • Anticancer
  • Antiproliferative
  • Azaindole
  • Cell cycle arrest
  • Citotoxicity

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