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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 32, Number 9
BKCSDE 32(9)
September 20, 2011 

Chalcones as Novel Non-peptidic μ-Calpain Inhibitors
Eunyoung Lee, Inhye Jang, Min Jung Shin, Hee-Ju Cho, Jungsook Kim, Ji-Eun Eom, Youngjoo Kwon*, Younghwa Na*,
Chalcone, Calpain inhibitor, Cathepsin B & L
In order to extend the scaffold of non-peptidic calpain inhibitor, we have designed and synthesized 14 chalcone derivatives categorized into two groups based on their structures. Compounds 7 (IC50 = 16.67 ± 0.42 μM) and 8 (IC50 = 16.92 ± 0.14 μM) in group A were most selective μ-calpain inhibitor over cathepsins B and L. On the other hand, compound 14 possessing furan ring exhibited inhibitory activities for μ-calpain (IC50 = 15.39 ± 1.34 μM) as well as cathepsin B (IC50 = 20.59 ± 1.35 μM). The results discovered implicated that chalcone analogues possessing proper size and functional groups can be a potential lead core for selective non-peptidic μ-calpain inhibitor. Furthermore, dual inhibitors for μ-calpain and cathepsin B can also be developed from chalcones by elaborate structure manipulation.
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