Novel 3-arylethynyl-substituted thieno[3,4-b]pyrazine derivatives as human transglutaminase 2 inhibitors?

Organic & Biomolecular Chemistry Pub Date: 2014-04-17 DOI: 10.1039/C4OB00179F

Abstract

In the process of optimization, we developed a novel core skeleton of thieno[3,4-b]pyrazine viaGK-13. The derivatives synthesized were shown to inhibit TGase 2 activity in cancer cells. Some of the hit compounds such as the arylethynyl group-coupled thieno[3,4-b]pyrazine derivatives were shown to exhibit promising activity for use as potential therapeutic small-molecules in renal cancer by inhibiting TGase 2 activity.

Graphical abstract: Novel 3-arylethynyl-substituted thieno[3,4-b]pyrazine derivatives as human transglutaminase 2 inhibitors
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