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Discovery and kinetic evaluation of 6-substituted 4-benzylthio-1,3,5- triazin-2(1H)-ones as inhibitors of cathepsin B
Sosič, Izidor ...
Cathepsin B is a lysosomal cysteine protease that has various physiological and pathophysiological functions. We present here the discovery of 6-substituted 4-benzylthio-1,3,5-triazin-2(1H)-ones as ...inhibitors of cathepsin B, starting from screening of a library of variously 2,4,6-trisubstituted 1,3,5-triazines and 1,3,5-triazin-2(1H)-ones on three different human cathepsins. The synthesis and enzymatic evaluation of a focused library of new 1,3,5-triazin-2(1H)-ones is also described. The detailed kinetics analyses have shown that these compounds can act as reversible, partial mixed-type inhibitors of cathepsin B, with Ki and Ki' values in the low micromolar range. The inhibitory activities of selected compounds were also assessed against two related cysteine proteases, cathepsinH and cathepsin L, to estimate their selectivity; these compounds have a selective profile for catB and catL over catH. Highlights A focused library of 6-substituted 4-benzylthio-1,3,5-triazin-2(1H)-ones was synthesized. The compounds inhibited cathepsin B in the low micromolar range. The detailed kinetics analyses showed that these compounds act as reversible, partial mixed-type inhibitors of cathepsin B. Molecular docking predicted binding in the S1' and S2' subsites of the enzyme.
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