Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371407 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
Sixteen disubstituted 1,2,3-triazoles were prepared using the Huisgen cycloaddition reaction and evaluated as inhibitors against caspase-3. The two most potent inhibitors were found to be (S)-1-((1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-1H-1,2,3-triazol-4-yl)methyl)-5-((2-(methoxymethyl)pyrrolidin-1-yl)sulfonyl)indoline-2,3-dione (7f) and (S)-1-((1-benzyl-1H-1,2,3-triazol-5-yl)methyl)-5-((2-(methoxymethyl)pyrrolidin-1-yl)sulfonyl)indoline-2,3-dione (8g) with IC50-values of 17 and 9 nM, respectively. Lineweaver–Burk plots revealed that these two triazoles show competitive inhibitory mechanism against caspase-3.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Yang Jiang, Trond Vidar Hansen,