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

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

Affiliation

  • 1 Department of Chemistry, Merck Research Laboratories, 320 Bent Street, Cambridge, MA 02141, United States. zenghb@hotmail.com
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.

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