Design, Synthesis and Inhibitory Activity of Photoswitchable RET Kinase Inhibitors.

ABSTRACT: REarranged during Transfection (RET) is a transmembrane receptor tyrosine kinase required for normal development and maintenance of neurons of the central and peripheral nervous systems. Deregulation of RET and hyperactivity of the RET kinase is intimately connected to several types of human cancers, most notably thyroid cancers, making it an attractive therapeutic target for small-molecule kinase inhibitors. Novel approaches, allowing external control of the activity of RET, would be key additions to the signal transduction toolbox. In this work, photoswitchable RET kinase inhibitors based on azo-functionalized pyrazolopyrimidines were developed, enabling photonic control of RET activity. The most promising compound displays excellent switching properties and stability with good inhibitor

SUBMITTER: Ferreira R 

PROVIDER: S-EPMC4421829 | biostudies-literature | 2015 May

REPOSITORIES: biostudies-literature