Boschelli, Diane H. published the artcileSynthesis and Src kinase inhibitory activity of a series of 4-phenylamino-3-quinolinecarbonitriles, HPLC of Formula: 2447-79-2, the publication is Journal of Medicinal Chemistry (2001), 44(5), 822-833, database is CAplus and MEDLINE.
Screening of a directed compound library in a yeast-based assay identified 4-[(2,4-dichlorophenyl)amino]-6,7-dimethoxy-3-quinolinecarbonitrile (I) as a Src inhibitor. An enzymic assay established that I was an ATP-competitive inhibitor of the kinase activity of Src. We present here SAR data for I which shows that the aniline group at C-4, the carbonitrile group at C-3, and the alkoxy groups at C-6 and C-7 of the quinoline are crucial for optimal activity. Increasing the size of the C-2 substituent of the aniline at C-4 of I from chloro to bromo to iodo resulted in a corresponding increase in Src inhibition. Furthermore, replacement of the 7-methoxy group of I with various 3-heteroalkylaminopropoxy groups provided increased inhibition of both Src enzymic and cellular activity. Compound II, which contains a 3-morpholinopropoxy group, had an IC50 of 3.8 nM in the Src enzymic assay and an IC50 of 940 nM for the inhibition of Src-dependent cell proliferation.
Journal of Medicinal Chemistry published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, HPLC of Formula: 2447-79-2.
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