期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 6, 页码 1626-1629出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.01.110
关键词
Caspase-3; Inhibitors; 1,2,3-Triazole; Isatin
资金
- Research Council of Norway
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 IC(50)-values of 17 and 9 nM, respectively. Lineweaver-Burk plots revealed that these two triazoles show competitive inhibitory mechanism against caspase-3. (C) 2011 Elsevier Ltd. All rights reserved.
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