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

  • Bioorg Med Chem Lett. 2011 Oct 1;21(19):5870-5. doi: 10.1016/j.bmcl.2011.07.101.
Hongbo Zeng  1 ,  David B Belanger ,  Patrick J Curran ,  Gerald W Shipps Jr ,  Hua Miao ,  Jack B Bracken ,  M Arshad Siddiqui ,  Michael Malkowski ,  Yan Wang
Affiliations
  • 1. Department of Chemistry, Merck Research Laboratories, 320 Bent Street, Cambridge, MA 02141, United States. [email protected]
PMID: 21855335 DOI: 10.1016/j.bmcl.2011.07.101
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.

Products