Discovery of novel 2-hydroxydiarylamide derivatives as TMPRSS4 inhibitors.

Bioorg Med Chem Lett 2013 Mar 8;23(6):1748-51. Epub 2013 Feb 8.

Biomedical Proteomics Research Center, Korea Research Institute of Bioscience and Biotechnology, Daejon 305-806, Republic of Korea.

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.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2013.01.055DOI Listing
March 2013

Publication Analysis

Top Keywords

serine protease
12
2-hydroxydiarylamide derivatives
8
cancer cells
8
colon cancer
8
tmprss4 serine
8
tmprss4
5
protease activity
4
activity suppressing
4
suppressing cancer
4
inhibiting tmprss4
4
synthesized evaluated
4
study novel
4
cells study
4
series 2-hydroxydiarylamide
4
derivatives synthesized
4
cancer cell
4
evaluated inhibiting
4
invasion derivatives
4
anti-invasive activity
4
promising anti-invasive
4

Altmetric Statistics

Similar Publications