863029-97-4

Upstream product

• 214470-68-5 7-(3-chloro-propoxy)-4-chloro-6-methoxy-quinoline-3-carbonitrile 
• 133303-88-5 3-chloro-4-(1-methyl-1H-imidazol-2-ylsulfanyl)phenylamine 
• 350-30-1 3-chloro-4-fluoronitrobenzene 
• 133303-87-4 2-(2-chloro-4-nitro-phenylsulfanyl)-1-methyl-1H-imidazole 

Downstream Products

• 263171-01-3 4-{3-chloro-4-[(1-methyl-1H-imidazol-2-yl)sulfanyl]anilino}-6-methoxy-7-[3-(4-morpholinyl)propoxy]-3-quinolinecarbonitrile 
• 863030-23-3 4-{3-chloro-4-[(1-methyl-1H-imidazole-2-yl)sulfanyl]anilino}-6-methoxy-7-{3-[4-(1-pyrrolidinyl)-1-piperidinyl]propoxy}-3-quinolinecarbonitrile 

Relevant academic research and scientific papers

3-Quinolinecarbonitrile protein kinase inhibitors

This invention provides a compound of Formula 1 where Ar, X, R1, R2, R3, and R4 are defined herein, or a pharmaceutically acceptable salt thereof useful in the prevention or inhibition of diseases associated wit

Synthesis and evaluation of 4-anilino-6, 7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade

4-[3-Chloro-4-(1-methyl-1H-imidazol-2-ylsulfanyl)]anilino-6, 7-diethoxy-3-quinolinecarbonitrile (3) was identified as a MEK1 kinase inhibitor with exceptional activity against LoVo cells. The structure-activity relationships of the C-4 aniline substituents were explored, and water-solubilizing groups were added at the C-7 position to improve physical properties. Secondary cellular assays revealed that a compound possessing the appropriate aniline substituents inhibited MEK1 as well as MAPK phosphorylation, thereby acting as a dual inhibitor of the Ras-MAPK signaling cascade.