Design and Synthesis of Novel Pyrazolopyrazinone Derivatives Targeting Lung Cancer Cells (A549)

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Kuzu E., Tan Uygun M.

11th International Drug Chemistry Conference, Antalya, Turkey, 9 - 12 March 2023, pp.102

  • Publication Type: Conference Paper / Summary Text
  • City: Antalya
  • Country: Turkey
  • Page Numbers: pp.102
  • Van Yüzüncü Yıl University Affiliated: Yes


Nitrogen-containing heterobicyclic systems are in the framework of many therapeutic agents. Among the heterobicyclic ring systems, various derivatives fused with pyrazole moiety are reported in the literature to act by inhibiting proliferation in cancer cells. It was found that the pyrazolopyrazine skeleton, which is one of the compounds formed by fusing with the pyrazole moiety, has a very high antiproliferative effect, especially in the lung cancer cell line.1 For example, Compound 1, causes apoptotic cell death in A549 lung cancer cell line (IC50: 24.2 µM); compound 2 was able to selectively inhibit the growth of lung cancer cells (H322, IC50: 28.5 µM) in a dose-dependent manner (Fig 1).2,3