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- W2017310317 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 (<TEX>$IC_{50}=16.67{pm}0.42{mu}M$</TEX>) and 8 (<TEX>$IC_{50}=16.92{pm}0.14{mu}M$</TEX>) in group A were most selective <TEX>${mu}$</TEX>-calpain inhibitor over cathepsins B and L. On the other hand, compound 14 possessing furan ring exhibited inhibitory activities for <TEX>${mu}$</TEX>-calpain (<TEX>$IC_{50}=15.39{pm}1.34{mu}M$</TEX>) as well as cathepsin B (<TEX>$IC_{50}=20.59{pm}1.35{mu}M$</TEX>). The results discovered implicated that chalcone analogues possessing proper size and functional groups can be a potential lead core for selective non-peptidic <TEX>${mu}$</TEX>-calpain inhibitor. Furthermore, dual inhibitors for <TEX>${mu}$</TEX>-calpain and cathepsin B can also be developed from chalcones by elaborate structure manipulation." @default.
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- W2017310317 date "2011-09-20" @default.
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- W2017310317 title "Chalcones as Novel Non-peptidic μ-Calpain Inhibitors" @default.
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- W2017310317 doi "https://doi.org/10.5012/bkcs.2011.32.9.3459" @default.
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