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 ( …

…, C Liang, Y Zhou, A Nematalla, X Wang, H Chen…

Index: Sun; Cui, Jean; Liang, Congxin; Zhou, Yong; Nematalla, Asaad; Wang, Xueyan; Chen, Hui; Tang, Cho; Wei, James Bioorganic and medicinal chemistry letters, 2002 , vol. 12, # 16 p. 2153 - 2157

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Citation Number: 22

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.