Potent and selective EGFR inhibitors based on 5-aryl-7H-pyrrolopyrimidin-4-amines
Reiersølmoen, Ann Christin; Aarhus, Thomas Ihle; Eckelt, Sarah; Nørsett, Kristin Gabestad; Sundby, Eirik; Hoff, Bård Helge
Journal article, Peer reviewed
Published version
Permanent lenke
http://hdl.handle.net/11250/2635253Utgivelsesdato
2019Metadata
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- Institutt for kjemi [1399]
- Institutt for materialteknologi [2553]
- Publikasjoner fra CRIStin - NTNU [38525]
Originalversjon
10.1016/j.bioorg.2019.102918Sammendrag
The epidermal growth factor receptor represents an important target in cancer therapy, and low molecular weight inhibitors based on quinazolines have reached the marked. Herein we report on a new scaffold, 5-aryl-7H-pyrrolo[2,3-d]pyrimidin-4-amines, and show that when employing (S)-phenylglycinol as C-4 substituent, potent inhibitors can be made. The two most active inhibitors have suitable druglike properties, were equipotent with Erlotinib in Ba/F3 cell studies, and showed lower cross reactivity than Erlotinib in a panel of 50 kinases.