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Chalcones as novel non-peptidic μ-calpain inhibitors

Title
Chalcones as novel non-peptidic μ-calpain inhibitors
Authors
Lee E.Jang I.Shin M.J.Cho H.-J.Kim J.Eom J.-E.Kwon Y.Na Y.
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2011
Journal Title
Bulletin of the Korean Chemical Society
ISSN
0253-2964JCR Link
Citation
vol. 32, no. 9, pp. 3459 - 3464
Indexed
SCI; SCIE; SCOPUS; KCI WOS scopus
Abstract
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 (IC 50 = 16.67 ± 0.42 μM) and 8 (IC 50 = 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 (IC 50 = 15.39 ± 1.34 μM) as well as cathepsin B (IC 50 = 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.
DOI
10.5012/bkcs.2011.32.9.3459
Appears in Collections:
약학대학 > 약학과 > Journal papers
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