title: Isatin 1,2,3-triazoles as potent inhibitors against caspase-3.
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 IC(50)-values of 17 and 9 nM, respectively. Lineweaver-Burk plots revealed that these two triazoles show competitive inhibitory mechanism against caspase-3.
authors.affiliation: School of Pharmacy, Department of Pharmaceutical Chemistry, University of Oslo, Oslo, Norway. yang.jiang@farmasi.uio.no
authors.forename: Yang
authors.initials: Y
authors.lastname: Jiang
authors.forename: Trond Vidar
authors.initials: TV
authors.lastname: Hansen
mesh_terms: D061945:Caspase Inhibitors; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D007510:Isatin / Q000737:chemistry*; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D061945:Caspase Inhibitors; D004791:Enzyme Inhibitors; D014230:Triazoles; D007510:Isatin