Jiangli Song

TL;DR: A series of thiosemicarbazone analogs based on the benzophenone, thiophene, pyridine, and fluorene molecular frameworks has been prepared by chemical synthesis and evaluated as small-molecule inhibitors of the cysteine proteases cathepsin L and cat hepsin B.

TL;DR: 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.

TL;DR: An important extension of this work designed to explore fused aryl-alkyl ring molecular systems that feature nitrogen atom incorporation and carbon atom exclusivity is reported, which establishes a high degree (>20-fold) of selectivity for the most active cathepsin L inhibitors in this series.

TL;DR: Active members of this structurally diverse group of benzoylbenzophenone thiosemicarbazone cathepsin L inhibitors show promise as potential anti-metastatic, pre-clinical drug candidates.

TL;DR: In this article, a compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathemsin K or cathephin L, will be therapeutically useful.