Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives.

@article{Mowafy2016TowardDO,
  title={Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives.},
  author={Samar Mowafy and Athanassios Galanis and Zainab M. Doctor and Raymond M. Paranal and Deena S. Lasheen and Nahla Ahmed Farag and Pasi A. J{\"a}nne and Khaled A M Abouzid},
  journal={Bioorganic & medicinal chemistry},
  year={2016},
  volume={24 16},
  pages={
          3501-12
        }
}
  • Samar Mowafy, Athanassios Galanis, +5 authors Khaled A M Abouzid
  • Published in
    Bioorganic & medicinal…
    2016
  • Chemistry, Medicine
  • A new series of 4-anilinoquinazolines with C-6 ureido and thioureido side chains and various substituents at the C-4 anilino moiety was designed, synthesized and evaluated as wild type (WT) and mutant EGFR inhibitors. Most of the compounds inhibited EGFR kinase wild type (EGFR WT) with IC50 values in the low nanomolar range (<0.495-9.05nM) and displayed more potent cytotoxic effect in BaF/3 expressing EGFR WT than reference compound gefitinib. The anti-proliferative effect of all synthesized… CONTINUE READING

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