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article · RSC Medicinal Chemistry

Design, synthesis and biological evaluation of novel morpholinopyrimidine-5-carbonitrile derivatives as dual PI3K/mTOR inhibitors

Abstract

values of 0.83 ± 0.05 and 2.85 ± 0.17 μM, respectively. Annexin-V and propidium iodide (PI) double labeling showed that compounds 12b and 12d promote cytotoxic leukemia SR apoptosis. Compounds 12b and 12d also caused a G2/M cell cycle arrest in the leukaemia SR cell line. The findings of this study indicate that the highest effect was observed for 12b, which was supported by western blot and docking analysis.

Research topics

  • Synthesis and biological activity
  • PI3K/AKT/mTOR signaling in cancer
  • Synthesis of Organic Compounds

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DOI: 10.1039/d3md00693j

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