869223-94-9

Upstream product

• 220509-98-8 5-(2-phenoxymethyl-pyrrolidine-1-sulfonyl)-1H-indole-2,3-dione 
• 504-63-2 trimethyleneglycol 

Downstream Products

• 869223-95-0 3-{2'-oxospiro[1,3-dioxane-1,3'-[3H]indol]-5'-(1-[(2S)-phenoxymethyl]-pyrrolidinylsulfonyl)}propanenitrile 
• 1150639-53-4 (S)-1-{[1'-[4-(2-bromo-ethoxy)-benzyl]-1',2'-dihydro-2'-oxospiro(1,3-dioxane-2,3'-[3H]indol)-5'-yl]sulfonyl}-2-(phenoxymethyl)-pyrrolidine 
• 1150639-54-5 (S)-1-{[1'-[4-(acetoxy)-benzyl]-1',2'-dihydro-2'-oxospiro(1,3-dioxane-2,3'-[3H]indol)-5'-yl]sulfonyl}-2-(phenoxymethyl)-pyrrolidine 
• 869223-97-2 2,2-dimethyl-3-[2'-oxo-5'-{[(2S)-2-(phenoxymethyl)pyrrolidin-1-yl]sulfonyl}spiro[1,3-dioxane-2,3'-indol]-1'(2'H)-yl]propanenitrile 
• 1202497-86-6 1-([2'-oxo-5'-([(2S)-2-(phenoxymethyl)pyrrolidin-1-yl]sulfonyl)spiro[1,3-dioxane-2,3'-indol]-1'(2'H)-yl]methyl)cyclobutanecarbonitrile 
• 1202497-87-7 1-([2'-oxo-5'-([(2S)-2-(phenoxymethyl)pyrrolidin-1-yl]sulfonyl)spiro[1,3-dioxane-2,3'-indol]-1'(2'H)-yl]methyl)cyclopentanecarbonitrile 
• 1202497-88-8 1-([5'-([(2S)-2-(phenoxymethyl)pyrrolidin-1-yl]sulfonyl)-2'-oxospiro[1,3-dioxane-2,3'-indol]-1'(2'H)-yl]methyl)cyclohexanecarbonitrile 

Relevant academic research and scientific papers

[18F]- and [11C]-Labeled N-benzyl-isatin sulfonamide analogues as PET tracers for Apoptosis: Synthesis, radiolabeling mechanism, and in vivo imaging study of apoptosis in Fas-treated mice using [ 11C]WC-98

The radiolabeled isatin sulfonamide caspase-3 inhibitor, [18F]2 (WC-II-89), is a potential PET radiotracer for noninvasive imaging of apoptosis. The radiolabeling mechanism was studied by 13C NMR, ESI/MS, and computational calculatio

3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3

Cysteine-dependant aspartyl protease (caspase) activation has been implicated as a part of the signal transduction pathway leading to apoptosis. It has been postulated that caspase-3 inhibition could attenuate cell damage after an ischemic event and thereby providing for a novel neuroprotective treatment for stroke. As part of a program to develop a small molecule inhibitor of caspase-3, a novel series of 3,4-dihydropyrimido(1,2-a)indol-10(2H)-ones (pyrimidoindolones) was identified. The synthesis, biological evaluation and structure-activity relationships of the pyrimidoindolones are described.

Pyrimidoindolones and methods for using same

Novel pyrimidoindolone compounds are disclosed. Methods of using the pyrimidoindolone compounds and compositions containing the compounds in the treatment and/or prevention of disease and other conditions related to inflammation, neurodegeneration, osteoarthritis and apoptosis are also disclosed.