Novel inhibitor of epidermal growth factor receptor (EGFR) and application thereof

2011 
The invention relates to a novel inhibitor of an EGFR and an application thereof. The general formula of the EGFR inhibitor is represented by a formula shown in the specification. In the formula, L is a C1-4 lower alkyl group, a C1-4 lower alkyloxy group, a C1-4 lower alkylamino group, O, OR4, S, SR4, NH or NR4, wherein R4 is a C1-4 lower alkyl group, a C1-4 lower alkyloxy group, or a C1-4 lower monoalkylamino group; R1 is a phenyl group, a substituted phenyl group, a substituted five-nine-membered aromatic cycle, a substituted five-nine-membered aromatic heterocycle or a substituted aromatic bicycle; R2 is hydrogen, a C1-9 alkyl group, a C1-9 alkyloxy group, OH, NH2, NO2, SH, or NR5R6, wherein R5R6 is hydrogen, a C1-9 alkyl group, a C1-9 alkyloxy group or a C1-9 monoalkylamino group, a three-nine-membered substituted aliphatic cycle, an aliphatic heterocycle, a substituted aromatic cycle, a substituted aromatic heterocycle, or a three-nine-membred bicycle; and R3 is halogen, H, SH, OH or NO2. The virtual screening of a computer, EGFR kinase activity inhibition experiments, and cancer cell inhibition experiments confirm that compounds of above formula are the EGFR inhibitor and have good curative effects and prevention effects on cancers related with the EGFR.
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