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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor
Journal of Medicinal Chemistry, Volume 53, No. 7, Year 2010
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Description
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. © 2010 American Chemical Society.
Authors & Co-Authors
Pawar, Vijaykumar
Germany, Dortmund
Chemical Genomics Centre of the Max Planck Society
Sos, Martin L.
Germany, Koln
Universität zu Köln
Rode, Haridas B.
Germany, Dortmund
Chemical Genomics Centre of the Max Planck Society
Rabiller, Matthias
Germany, Dortmund
Chemical Genomics Centre of the Max Planck Society
Heynck, Stefanie
Germany, Koln
Universität zu Köln
van Otterlo, Willem A. L.
Germany, Dortmund
Chemical Genomics Centre of the Max Planck Society
South Africa, Johannesburg
University of the Witwatersrand
Thomas, Roman K.
Germany, Dortmund
Chemical Genomics Centre of the Max Planck Society
Germany, Koln
Universität zu Köln
Rauh, Daniel F.
Germany, Dortmund
Chemical Genomics Centre of the Max Planck Society
Statistics
Citations: 55
Authors: 8
Affiliations: 3
Identifiers
Doi:
10.1021/jm901877j
ISSN:
00222623
e-ISSN:
15204804
Research Areas
Cancer