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Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line
Authors:Junsang Lee  Bong Soo Nam  Hwan Kim  Chang-Hyun Oh  So Ha Lee  Seung Joo Cho  Tae Bo Sim  Jung-Mi Hah  Dong Jin Kim  Jinsung Tae  Kyung Ho Yoo
Affiliation:1. Life/Health Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea;2. Department of Chemistry, Yonsei University, Seodaemun-gu, Seoul 120-749, Republic of Korea;3. Research Center for Resistant Cells, Chosun University, Gwangju 501-759, Republic of Korea;4. Department of Cellular and Molecular Medicine, College of Medicine, Chosun University, 375 Seosuk-dong, Dong-gu Gwangju 501-759, Republic of Korea
Abstract:
The synthesis of a novel series of aminoquinazoline derivatives 1ar 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.
Keywords:
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