Bulletin of the Korean Chemical Society

  • 제32권9호
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  • Pages.3459-3464
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  • 2011
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  • 0253-2964(pISSN)
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  • 1229-5949(eISSN)
대한화학회 (Korean Chemical Society)
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Chalcones as Novel Non-peptidic μ-Calpain Inhibitors

  • Lee, Eun-Young (College of Pharmacy & Division of Life & Pharmaceutical Sciences, Ewha Womans University) ;
  • Jang, In-Hye (College of Pharmacy, Catholic University of Daegu) ;
  • Shin, Min-Jung (College of Pharmacy, Catholic University of Daegu) ;
  • Cho, Hee-Ju (College of Pharmacy, Catholic University of Daegu) ;
  • Kim, Jung-Sook (College of Pharmacy, CHA University) ;
  • Eom, Ji-Eun (College of Pharmacy & Division of Life & Pharmaceutical Sciences, Ewha Womans University) ;
  • Kwon, Young-Joo (College of Pharmacy & Division of Life & Pharmaceutical Sciences, Ewha Womans University) ;
  • Na, Young-Hwa (College of Pharmacy, CHA University)
  • 투고 : 2011.07.21
  • 심사 : 2011.08.02
  • 발행 : 2011.09.20
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초록

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 ($IC_{50}=16.67{\pm}0.42{\mu}M$) and 8 ($IC_{50}=16.92{\pm}0.14{\mu}M$) in group A were most selective ${\mu}$-calpain inhibitor over cathepsins B and L. On the other hand, compound 14 possessing furan ring exhibited inhibitory activities for ${\mu}$-calpain ($IC_{50}=15.39{\pm}1.34{\mu}M$) as well as cathepsin B ($IC_{50}=20.59{\pm}1.35{\mu}M$). The results discovered implicated that chalcone analogues possessing proper size and functional groups can be a potential lead core for selective non-peptidic ${\mu}$-calpain inhibitor. Furthermore, dual inhibitors for ${\mu}$-calpain and cathepsin B can also be developed from chalcones by elaborate structure manipulation.

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피인용 문헌

  1. Identification of Chalcones as Fasciola hepatica Cathepsin L Inhibitors Using a Comprehensive Experimental and Computational Approach vol.10, pp.7, 2016, https://doi.org/10.1371/journal.pntd.0004834
  2. Bioinspired Diastereoconvergent Synthesis of the Tricyclic Core of Palodesangrens via Diels-Alder Reaction, LiAlH4-Mediated Isomerization, and Acid-Mediated Cyclization vol.83, pp.9, 2011, https://doi.org/10.1021/acs.joc.8b00668