Synthesis and biochemical evaluation of thiochromanone thiosemicarbazone analogues as inhibitors of cathepsin L

…, GE Chavarria, AK Charlton-Sevcik…

文献索引：Song, Jiangli; Jones, Lindsay M.; Kumar, G. D. Kishore; Conner, Elizabeth S.; Bayeh, Liela; Chavarria, Gustavo E.; Charlton-Sevcik, Amanda K.; Chen, Shen-En; Chaplin, David J.; Trawick, Mary Lynn; Pinney, Kevin G. ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 6 p. 450 - 453

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被引用次数: 11

摘要

A series of 36 thiosemicarbazone analogues containing the thiochromanone molecular scaffold functionalized primarily at the C-6 position were prepared by chemical synthesis and evaluated as inhibitors of cathepsins L and B. The most promising inhibitors from this group are selective for cathepsin L and demonstrate IC50 values in the low nanomolar range. In nearly all cases, the thiochromanone sulfide analogues show superior inhibition ...