Potent and selective EGFR inhibitors based on 5-aryl-7H-pyrrolopyrimidin-4-amines

Link:
Autor/in:
Erscheinungsjahr:
2019
Medientyp:
Text
Schlagworte:
  • Pyrrolopyrimidine
  • EGFR
  • Erlotinib
  • Kinase
  • Chiral drug
  • ()-phenylglycinol
Beschreibung:
  • 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.
Lizenz:
  • info:eu-repo/semantics/openAccess
Quellsystem:
Forschungsinformationssystem der UHH

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Quelldatensatz
oai:www.edit.fis.uni-hamburg.de:publications/99361556-bf80-4f35-8387-4433112c322a