Title of article :
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(p185erbB) tyrosine kinases
Author/Authors :
Li Sun، نويسنده , , Jingrong Jean Cui، نويسنده , , Congxin Liang، نويسنده , , Yong Zhou، نويسنده , , Asaad Nematalla، نويسنده , , Xueyan Wang، نويسنده , , Hui Chen، نويسنده , , Cho Tang، نويسنده , , James Wei، نويسنده ,
Abstract :
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.
