Bioorganic and medicinal chemistry letters p. 2153 - 2157 (2002)
Update date:2022-08-05
Topics:
Sun
Cui, Jean
Liang, Congxin
Zhou, Yong
Nematalla, Asaad
Wang, Xueyan
Chen, Hui
Tang, Cho
Wei, James
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 (p185(erbB)). Structure-activity relationships (SARs) for this class of compounds are presented.
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Doi:10.1021/acs.orglett.8b02929
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