3,5-Disubstituted quinolines as novel c-Jun N-terminal kinase inhibitors.

Article Details

Citation

Copy to clipboard

Jiang R, Duckett D, Chen W, Habel J, Ling YY, LoGrasso P, Kamenecka TM

3,5-Disubstituted quinolines as novel c-Jun N-terminal kinase inhibitors.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6378-82. Epub 2007 Aug 26.

PubMed ID

17911023 [ View in PubMed

]

Abstract

The structure-based design and synthesis of a novel series of c-Jun N-terminal kinase (JNK) inhibitors with selectivity against p38 is reported. The unique structure of 3,5-disubstituted quinolines (2) was developed from the previously reported 4-(2,7-phenanthrolin-9-yl)phenol (1). The X-ray crystal structure of 16a in JNK3 reveals an unexpected binding mode for this new scaffold with protein.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
9-(4-Hydroxyphenyl)-2,7-Phenanthroline	Mitogen-activated protein kinase 10	IC 50 (nM)	590	N/A	N/A	Details
N-(tert-butyl)-4-[5-(pyridin-2-ylamino)quinolin-3-yl]benzenesulfonamide	Mitogen-activated protein kinase 10	IC 50 (nM)	150	N/A	N/A	Details