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 represent...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-10, Vol.20 (19), p.5722-5725
Hauptverfasser: Lee, Junsang, Nam, Bong Soo, Kim, Hwan, Oh, Chang-Hyun, Lee, So Ha, Cho, Seung Joo, Sim, Tae Bo, Hah, Jung-Mi, Kim, Dong Jin, Tae, Jinsung, Yoo, Kyung Ho
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Sprache:eng
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Zusammenfassung: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. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.08.010