Design and Synthesis of 4‐Anilinothieno[2,3‐d]pyrimidine‐Based Compounds as Dual EGFR/HER‐2 Inhibitors

@article{Hadi2016DesignAS,
  title={Design and Synthesis of 4‐Anilinothieno[2,3‐d]pyrimidine‐Based Compounds as Dual EGFR/HER‐2 Inhibitors},
  author={Soha R Abd El Hadi and Deena S. Lasheen and M. Hassan and K. A. Abouzid},
  journal={Archiv der Pharmazie},
  year={2016},
  volume={349}
}
  • Soha R Abd El Hadi, Deena S. Lasheen, +1 author K. A. Abouzid
  • Published 2016
  • Chemistry, Medicine
  • Archiv der Pharmazie
  • Dual inhibition of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER‐2) is an attractive cancer therapeutic approach. In this study, new series of 4‐anilinothieno[2,3‐d]pyrimidines were designed, synthesized, and tested as dual EGFR/HER‐2 kinase inhibitors. Five compounds (8a, 8b, 8e–g) demonstrated low to submicromolar inhibition of both kinases with IC50 values of 1.2, 0.6, 0.3, 0.2, 0.4 μM and 8.2, 3.4, 1.3, 0.5, 2.7 μM for the EGFR and HER‐2… CONTINUE READING
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