Benzopyrimidodiazepinone inhibitors of TNK2

Bioorg Med Chem Lett. 2020 Feb 15;30(4):126948. doi: 10.1016/j.bmcl.2020.126948.

Brian J Groendyke ¹, Chelsea E Powell ¹, Frederic Feru ¹, Thomas W Gero ¹, Zhengnian Li ¹, Hilary Szabo ², Kevin Pang ³, John Feutrill ⁴, Bailing Chen ⁴, Bin Li ⁴, Nathanael S Gray ¹, David A Scott ¹

Affiliations

1 Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02115, USA; Department of Biological Chemistry & Molecular Pharmacology, Harvard Medical School, 360 Longwood Ave, Boston, MA 02115, USA.
2 Vivid BioSciences, 50 Northern Ave, Boston, MA 02210, USA.
3 Northeastern University, 360 Huntington Ave, Boston, MA 02115, USA.
4 SYNthesis Med Chem, 425 Changyang Street, Suzhou Industry Park, Suzhou, Jiangsu, China.

PMID: 31928839 DOI: 10.1016/j.bmcl.2020.126948

Abstract

The SAR of a series of benzopyrimidodiazepinone inhibitors of TNK2 was developed, starting from the potent and selective compound XMD8-87. A diverse set of anilines was introduced in an effort to improve the in vivo PK profile and minimize the risk of quinone diimine formation.

Keywords

Benzopyrimidodiazepinone; Kinase inhibitor; TNK2.

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