Discovery of novel 2-hydroxydiarylamide derivatives as TMPRSS4 inhibitors

作者：Kang Sunghyun; Min Hye Jin; Kang Min Seo; Jung Myung Geun; Kim Semi^*

来源：Bioorganic & Medicinal Chemistry Letters, 2013, 23(6): 1748-1751.

DOI：10.1016/j.bmcl.2013.01.055

• 2-Hydroxydiarylamide
• TMPRSS4 inhibitors
• Invasion
• Antitumor

TMPRSS4 is a novel type II transmembrane serine protease that has been implicated in the invasion and metastasis of colon cancer cells. In this study, a novel series of 2-hydroxydiarylamide derivatives were synthesized and evaluated for inhibiting TMPRSS4 serine protease activity and suppressing cancer cell invasion. These derivatives demonstrated good inhibitory activity against TMPRSS4 serine protease, which correlated with the promising anti-invasive activity of colon cancer cells overexpressing TMPRSS4.

• 出版日期2013-3-15