Systematically Mitigating the p38α Activity of Triazole-based BET Inhibitors.

The Bromodomain and Extra Terminal (BET) family of proteins recognize post-translational -ε-acetylated lysine modifications, regulating transcription as "reader" proteins. Bromodomain inhibitors are interesting targets for the development of potential cancer, inflammation, and heart disease treatments. Several dual kinase-bromodomain inhibitors have been identified by screening kinase inhibitor libraries against BET proteins.

Regiocontrolled Wacker Oxidation of Cinnamyl Azides.

A highly regioselective Wacker oxidation has been developed for the oxidation of cinnamyl azides. The catalytic oxidation tolerates the azide functionality, and more than 15 β-azido ketones were isolated (25-92% yield). High regioselectivity for the aryl ketone is observed in all cases.