ABSTRACT
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.
Subject(s)
Antineoplastic Agents/chemical synthesis , Chromones/chemical synthesis , Quinazolines/chemistry , Antineoplastic Agents/chemistry , Antineoplastic Agents/therapeutic use , Cell Line, Tumor , Chromones/chemistry , Chromones/therapeutic use , Humans , Melanoma/drug therapy , Quinazolines/chemical synthesis , Quinazolines/therapeutic use , Structure-Activity RelationshipABSTRACT
The synthesis of a novel series of aminoquinoline derivatives 1a-p and their antiproliferative activities against A375 human melanoma cell line were described. Most compounds showed superior antiproliferative activities to Sorafenib as a reference compound. Among them, quinolinyloxymethylphenyl compounds 1k and 1l exhibited potent activities (IC(50)=0.77 and 0.79microM, respectively) and excellent selectivity against melanoma and fibroblast cell lines.
