170108-12-0

Upstream product

• 302-17-0 chloral hydrate 
• 4519-40-8 2,3-difluoroanilline 

Downstream Products

• 158580-95-1 6,7-difluoro-1H-indole-2,3-dione 
• 1491155-51-1 3-(5-tert-butyl-2-hydroxyphenyl)-6,7-difluoro-3-(4-methoxyphenyl)-1,3-dihydro-2H-indol-2-one 
• 1491155-60-2 3-(5-tert-butyl-2-hydroxyphenyl)-6,7-difluoro-3-(4-hydroxyphenyl)-1,3-dihydro-2H-indol-2-one 
• 867155-10-0 6,7-difluoro-3-hydroxy-3-(4-methoxyphenyl)-1,3-dihydro-2H-indol-2-one 
• 1491155-36-2 3-[4-(dimethylamino)phenyl]-6,7-difluoro-3-hydroxy-1,3-dihydro-2H-indol-2-one 
• 1584229-89-9 3,3-bis(5-tert-butyl-2-hydroxyphenyl)-6,7-difluoroindolin-2-one 

Relevant academic research and scientific papers

3-3-DI-SUBSTITUTED-OXINDOLES AS INHIBITORS OF TRANSLATION INITIATION

Compositions and methods for inhibiting translation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using diaryloxindole compounds are described.

Synthesis and SAR study of novel 3,3-diphenyl-1,3-dihydroindol-2-one derivatives as potent eIF2·GTP·Met-tRNAiMet ternary complex inhibitors

The growing recognition of inhibition of translation initiation as a new and promising paradigm for mechanism-based anti-cancer therapeutics is driving the development of potent, specific, and druggable inhibitors. The 3,3-diaryloxindoles were recently reported as potential inhibitors of the eIF2·GTP·Met-tRNAiMet ternary complex assembly and 3-{5-tert-butyl-2-hydroxyphenyl}-3-phenyl-1,3-dihydro-2H-indol-2- one #1181 was identified as the prototypic agent of this chemotype. Herein, we report our continuous effort to further develop this chemotype by exploring the structural latitude toward different polar and hydrophobic substitutions. Many of the novel compounds are more potent than the parent compound in the dual luciferase ternary complex reporter assay, activate downstream effectors of reduced ternary complex abundance, and inhibit cancer cell proliferation in the low μM range. Moreover, some of these compounds are decorated with substituents that are known to endow favorable physicochemical properties and as such are good candidates for evaluation in animal models of human cancer.

4- [HETEROCYCLYL-METHYL] -8-FLUORO-QUINOLIN-2-ONES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS

Novel compounds of formulae (II, III) and pharmaceutical compositions have been found to inhibit inducible NOS synthase wherein: R4, R5, R6 and R7 are independently selected from the group consisting of hydrogen, lower alkyl, and halogen; and, R8 has the structure whrein X1, X2, X3, X4, X5, X6, R9, R13, R14 and n are as described herein.