Potent and selective EGFR inhibitors based on 5-aryl-7H-pyrrolopyrimidin-4-amines |
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| Institution: | 1. Department of Chemistry, Norwegian University of Science and Technology (NTNU), NO-7491 Trondheim, Norway;2. Department of Material Science, Norwegian University of Science and Technology (NTNU), NO-7491 Trondheim, Norway;3. Institute of Organic Chemistry, Universität Hamburg, Welckerstrasse 8, 201354 Hamburg, Germany;4. Department of Biomedical Laboratory Science, Norwegian University of Science and Technology (NTNU), NO-7491 Trondheim, Norway;5. Department of Computer Science, Norwegian University of Science and Technology (NTNU), NO-7491 Trondheim, Norway |
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| Abstract: | 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-pyrrolo2,3-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. |
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| Keywords: | Pyrrolopyrimidine EGFR Erlotinib Kinase Chiral drug |
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