516479-35-9

Upstream product

• 3516-87-8 ethyl 2,3,4,5,6-pentafluorobenzoylacetate 
• 122-51-0 orthoformic acid triethyl ester 

Downstream Products

• 448210-39-7 2-pentafluorobenzoyl-3-[N'-(pyridine-3-carbonyl)-hydrazino]-acrylic acid ethyl ester 
• 448210-37-5 2-pentafluorobenzoyl-3-[N'-(pyridine-4-carbonyl)-hydrazino]-acrylic acid ethyl ester 
• 448210-35-3 3-[N'-(3-nitro-benzoyl)-hydrazino]-2-pentafluorobenzoyl-acrylic acid ethyl ester 
• 119877-56-4 ethyl 5,6,7,8-tetrafluoro-4-oxo-1-(pentafluorophenyl)-1,4-dihydroquinoline-3-carboxylate 
• 448210-44-4 5,6,7,8-tetrafluoro-1-(3-nitro-benzoylamino)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid ethyl ester 
• 476005-98-8 1-(benzimidoyl-amino)-5,6,7,8-tetrafluoro-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

Inhibition of the signal transducer and activator of transcription-3 (STAT3) signaling pathway by 4-oxo-1-phenyl-1,4-dihydroquinoline-3-carboxylic acid esters

The JAK-STAT3 pathway regulates genes that are important in cell proliferation and thus is a promising target for cancer therapy. A high-throughput screening (HTS) campaign using an Apo-ONE Homogenous Caspase 3/7 assay in U266 cells identified 4-oxo-1-phenyl-1,4-dihydroquinoline-3-carboxylic acid ethyl ester 4 as a potential STAT3 pathway inhibitor. Optimization of this HTS hit led to the identification of the 7-cyano analogue 8, which inhibited STAT3-Y705 phosphorylation with an EC50 of 170 nM. Compound 8 also inhibited cytokine induced JAK activation but did not inhibit BCR-ABL activated STAT5 phosphorylation in K562 cells.

Aminoquinolones as GSK-3 inhibitors

Provided herein are aminoquinolones and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating, preventing or ameliorating GSK-3 mediated diseases.