Format

Send to

Choose Destination
Bioorg Chem. 2013 Dec;51:24-30. doi: 10.1016/j.bioorg.2013.09.002. Epub 2013 Sep 16.

Synthesis and investigation of dihydroxychalcones as calpain and cathepsin inhibitors.

Author information

1
College of Pharmacy, Graduate School of Pharmaceutical Sciences, Global Top5 Research Program, Ewha Womans University, Seoul 120-750, Republic of Korea.

Abstract

In order to identify potential calpain and cathepsin inhibitors we prepared 12 dihydroxychalcone analogues and tested their ability to inhibit μ-calpain, m-calpain, cathepsins B and L. In the calpain inhibition test, compound 10 exhibited the most active inhibitory activity against m-calpain with an IC50 value of 25.25±0.901μM. With respect to inhibition of cathepsins B and L, compound 13 exhibited the most potent inhibitory activity on cathepsin L and moderate inhibitory activity on cathepsin B with IC50 values of 2.80±0.100 and 11.47±0.087μM, respectively. Our results suggest the possibility of developing dual calpain and cathepsin inhibitors by properly modulating structures and/or combining the essential aspects of the functional group effective for specific calpain and cathepsin inhibition.

KEYWORDS:

Calpain inhibitor; Cathepsin B; Dihydroxychalcone; L Inhibitor

PMID:
24095934
DOI:
10.1016/j.bioorg.2013.09.002
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center