Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor.

Article Details

Citation
Copy to clipboard

Pawar VG, Sos ML, Rode HB, Rabiller M, Heynck S, van Otterlo WA, Thomas RK, Rauh D

Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor.

J Med Chem. 2010 Apr 8;53(7):2892-901. doi: 10.1021/jm901877j.

PubMed ID
20222733 [ View in PubMed
]
Abstract

The mutant receptor tyrosine kinase EGFR is a validated and therapeutically amenable target for genotypically selected lung cancer patients. Here we present the synthesis and biological evaluation of a series of 6- and 7-substituted 4-anilinoquinolines as potent type I inhibitors of clinically relevant mutant variants of EGFR. Quinolines 3a and 3e were found to be highly active kinase inhibitors in biochemical assays and were further investigated for their biological effect on EGFR-dependent Ba/F3 cells and non-small cell lung cancer (NSCLC) cell lines.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
ErlotinibEpidermal growth factor receptorIC 50 (nM)0.2N/AN/ADetails