Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family

…, A Hutchaleelaha, SJ Hollenbach, K Abe…

Index: Pandey, Anjali; Volkots, Deborah L.; Seroogy, Joseph M.; Rose, Jack W.; Yu, Jin-Chen; Lambing, Joseph L.; Hutchaleelaha, Athiwat; Hollenbach, Stanley J.; Abe, Keith; Giese, Neill A.; Scarborough, Robert M. Journal of Medicinal Chemistry, 2002 , vol. 45, # 17 p. 3772 - 3793

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Citation Number: 124

Abstract

We have previously found that the 4-[4-(N-substituted carbamoyl)-1-piperazinyl]-6, 7- dimethoxyquinazolines can function as potent and selective inhibitors of platelet-derived growth factor receptor (PDGFR) phosphorylation. A series of highly potent, specific, orally active, small molecule kinase inhibitors directed against members of PDGFR receptor have been developed through modifications of the novel quinazoline template I. Systematic ...