Chalcones as Novel Non-peptidic μ-Calpain Inhibitors 


Vol. 32,  No. 9, pp. 3459-3464, Sep.  2011
10.5012/bkcs.2011.32.9.3459


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  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 (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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  Cite this article

[IEEE Style]

E. Lee, I. Jang, M. J. Shin, H. Cho, J. Kim, J. Eom, Y. Kwon, Y. Na, "Chalcones as Novel Non-peptidic μ-Calpain Inhibitors," Bulletin of the Korean Chemical Society, vol. 32, no. 9, pp. 3459-3464, 2011. DOI: 10.5012/bkcs.2011.32.9.3459.

[ACM Style]

Eunyoung Lee, Inhye Jang, Min Jung Shin, Hee-Ju Cho, Jungsook Kim, Ji-Eun Eom, Youngjoo Kwon, and Younghwa Na. 2011. Chalcones as Novel Non-peptidic μ-Calpain Inhibitors. Bulletin of the Korean Chemical Society, 32, 9, (2011), 3459-3464. DOI: 10.5012/bkcs.2011.32.9.3459.

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ISSN(Print) 0253-2964
ISSN(Online) 1229-5949