Rational design of 4, 5-disubstituted-5, 7-dihydro-pyrrolo [2, 3-d] pyrimidin-6-ones as a novel class of inhibitors of epidermal growth factor receptor (EGF-R) and Her2 ( …
A novel class of 4, 5-disubstituted-5, 7-dihydro-pyrrolo [2, 3-d] pyrimidin-6-ones has been discovered as potent and selective inhibitors of the EGF-R tyrosine kinase family. These compounds selectively inhibit EGF-R kinase activity at low nanomolar concentration and tyrosine autophosphorylation in cells expressing EGF-R or Her2 (p185erbB). Structure– activity relationships (SARs) for this class of compounds are presented.
