1258203-07-4Relevant academic research and scientific papers
Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L
Kumar, G.D. Kishore,Chavarria, Gustavo E.,Charlton-Sevcik, Amanda K.,Yoo, Grace Kim,Song, Jiangli,Strecker, Tracy E.,Siim, Bronwyn G.,Chaplin, David J.,Trawick, Mary Lynn,Pinney, Kevin G.
supporting information; experimental part, p. 6610 - 6615 (2010/12/20)
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 cathepsin B. The two most potent inhibitors of cathepsin L in this series (IC50 50 = 150.8 nM). Bromine substitution in the thiophene series results in compounds that demonstrate only moderate inhibition of cathepsin L. The two most active analogs in the benzophenone thiosemicarbazone series are highly selective for their inhibition of cathepsin L versus cathepsin B.
