Potency switch between CHK1 and MK2: Discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors

doi:10.1016/j.bmcl.2013.03.100

Bioorganic & Medicinal Chemistry Letters

Volume 23, Issue 10, 15 May 2013, Pages 2863-2867

https://doi.org/10.1016/j.bmcl.2013.03.100 Get rights and content

Abstract

Chemistry has been developed to access both imidazo[1,2-a]pyrazines and imidazo[1,2-c]pyrimidines. Small structural modifications in both series led to a switch of potency between two kinases involved in mediating cell cycle checkpoint control, CHK1 and MK2.

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Acknowledgments

We thank Drs. John Piwinski and Neng-Yang Shih for support of this work.

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^†: Present address: Millennium: The Takeda Oncology Company, Cambridge, MA 02139, USA.

^‡: Present address: EnVivo Pharma Inc., Watertown, MA 02472, USA.

^§: Present address: Paraza Pharma Inc., Laval, Quebec, Canada, H7V 5B7.

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Potency switch between CHK1 and MK2: Discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors

Abstract

Graphical abstract

Section snippets

Acknowledgments

Genes Dev.

Nature

Curr. Opin. Cell Biol.

Cancer Res.

Annu. Rev. Biochem.

Science

Nature

Clin. Cancer Res.

Expert Opin. Ther. Pat.

Mol. Cancer Ther.

Mol. Cancer Ther.

Mol. Cancer Ther.