Balancing potency, metabolic stability and permeability in pyrrolopyrimidine-based EGFR inhibitors

The present study describes our continuous effort to develop epidermal growth factor receptor (EGFR) inhibitors based on the 6-aryl-pyrrolo[2,3-d]pyrimidin-4-amine scaffold. The activity-ADME space has been evaluated by synthesizing 43 new structures, including four variations of the 4-amino group a...

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Veröffentlicht in:	European journal of medicinal chemistry 2016-11, Vol.124, p.583-607
Hauptverfasser:	Han, Jin, Henriksen, Silje, Nørsett, Kristin G., Sundby, Eirik, Hoff, Bård Helge
Format:	Artikel
Sprache:	eng
Schlagworte:	ADME Cell Line Cell Proliferation - drug effects Drug Design Drug Stability EGFR Erlotinib Humans Inhibitory Concentration 50 Metabolism Models, Molecular Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - metabolism Pyrimidines - pharmacology Pyrroles - chemical synthesis Pyrroles - chemistry Pyrroles - metabolism Pyrroles - pharmacology Pyrrolopyrimidine Receptor, Epidermal Growth Factor - antagonists & inhibitors SAR Structure-Activity Relationship
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