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Issue 27, 2014
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Novel 3-arylethynyl-substituted thieno[3,4-b]pyrazine derivatives as human transglutaminase 2 inhibitors

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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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Publication details

The article was received on 23 Jan 2014, accepted on 17 Apr 2014, published on 17 Apr 2014 and first published online on 17 Apr 2014


Article type: Paper
DOI: 10.1039/C4OB00179F
Citation: Org. Biomol. Chem., 2014,12, 4932-4940
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    Novel 3-arylethynyl-substituted thieno[3,4-b]pyrazine derivatives as human transglutaminase 2 inhibitors

    N. Kim, S. H. Kwak, S. Lee, V. Juvekar, B. Lee, H. Ahn, S. Kim and Y. Gong, Org. Biomol. Chem., 2014, 12, 4932
    DOI: 10.1039/C4OB00179F

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