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

Add time:07/28/2019    Source:sciencedirect.com

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.

We also recommend Trading Suppliers and Manufacturers of 2-Methoxy-7H-pyrrolo[2,3-d]pyriMidin-4-aMine (cas 100383-13-9). Pls Click Website Link as below: cas 100383-13-9 suppliers

Prev:Lanthanide-catalyzed asymmetric 1,3-dipolar cycloaddition of nitrones to alkenes using 3,3′-bis(2-oxazolyl)-1,1′-bi-2-naphthol (BINOL-Box) ligands
Next:Structural and electronic properties of new fullerene derivatives and their possible application as HIV-1 protease inhibitors)