Discovery of novel quinazoline derivatives bearing semicarbazone moiety as potent EGFR kinase inhibitors

@inproceedings{Tu2018DiscoveryON,
  title={Discovery of novel quinazoline derivatives bearing semicarbazone moiety as potent EGFR kinase inhibitors},
  author={Yuanbiao Tu and Caolin Wang and Zunhua Yang and Bingbing Zhao and Luogen Lai and Qi Chang Yang and Pengwu Zheng and Wufu Zhu},
  booktitle={Computational and structural biotechnology journal},
  year={2018}
}
Aimed at discovering effective EGFR inhibitors, six series of quinazoline derivatives bearing a semicarbazone moiety were designed, synthesized and evaluated in different cancer cell lines (A549, HepG2, MCF-7 and PC-3). Most of the selected compounds showed remarkable cytotoxicity with IC50 values reaching the nanomole range. Further, the inhibition efficacy of 11 compounds against EGFR kinases was tested, which demonstrated excellent IC50 values in nanomolar level. Importantly, 2 compounds… CONTINUE READING

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