Discovery of novel imidazo [1, 2-a] pyrazin-8-amines as Brk/PTK6 inhibitors

…, H Miao, JB Bracken, MA Siddiqui, M Malkowski…

Index: Zeng, Hongbo; Belanger, David B.; Curran, Patrick J.; Shipps Jr., Gerald W.; Miao, Hua; Bracken, Jack B.; Arshad Siddiqui; Malkowski, Michael; Wang, Yan Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 19 p. 5870 - 5875

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Citation Number: 16

Abstract

A series of substituted imidazo [1, 2-a] pyrazin-8-amines were discovered as novel breast tumor kinase (Brk)/protein tyrosine kinase 6 (PTK6) inhibitors. Tool compounds with low- nanomolar Brk inhibition activity, high selectivity towards other kinases and desirable DMPK properties were achieved to enable the exploration of Brk as an oncology target.