Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line

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 (IC50 = 0.006 μM) and good selectivity over HS27 fibroblast cell line.

Graphical abstractThe 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 (IC50 = 0.006 μM) and good selectivity over HS27 fibroblast cell line.Figure optionsDownload full-size imageDownload as PowerPoint slide