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  • Title: New substituted 4-arylaminoquinazolines as potent inhibitors of breast tumor cell lines: in vitro and docking experiments.
    Author: de Oliveira AN, Bocca CC, Carvalho JE, Ruiz AL, Silva TP, Rittner R, Hoehr NF.
    Journal: Eur J Med Chem; 2010 Sep; 45(9):4339-42. PubMed ID: 20627376.
    Abstract:
    The arylquinazolines represent significant advances in the clinical management of breast cancer. Nevertheless some confirmatory studies must be considered to foster the use of anti-EGFR therapies including safety and clinical use. Two 4-arylaminoquinazoline derivatives, recently synthesized, were tested as kinase inhibitors and their citotoxicities showed potent growth inhibitory activity in breast tumor cell lines (MCF-7). The predicted complex structure of quinazoline inhibitors with EGFR protein from molecular docking provided a stereoview of the binding site correlated with structure activity, affording important information about structure-based drug design.
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