The synthesis of a novel series of aminoquinazoline derivatives 1a-r and their antiproliferative activities against A375 human melanoma cell line were described. Among them, six compounds showed superior antiproliferative activities to Sorafenib as a reference compound. In particular, the representative compound 1q bearing chromen-4-one moiety exhibited excellent antiproliferative activity (IC(50)=0.006 μM) and good selectivity over HS27 fibroblast cell line.

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http://dx.doi.org/10.1016/j.bmcl.2010.08.010DOI Listing

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