Synthesis and investigation of dihydroxychalcones as calpain and cathepsin inhibitors

Kyung Hye Baek, Radha Karki, Eung Seok Lee, Younghwa Na, Youngjoo Kwon

Research output: Contribution to journalArticlepeer-review

9 Scopus citations

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 ± 0.901 μM. 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 ± 0.087 μM, 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.

Original languageEnglish
Pages (from-to)24-30
Number of pages7
JournalBioorganic Chemistry
Volume51
DOIs
StatePublished - 2013

Keywords

  • B L Inhibitor
  • Calpain inhibitor
  • Cathepsin
  • Dihydroxychalcone

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