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

Authors
Lee, JunsangNam, Bong SooKim, HwanOh, Chang-HyunLee, So HaCho, Seung JooSim, Tae BoHah, Jung-MiKim, Dong JinTae, JinsungYoo, Kyung Ho
Issue Date
2010-10-01
Publisher
Pergamon Press Ltd.
Citation
Bioorganic & Medicinal Chemistry Letters, v.20, no.19, pp.5722 - 5725
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 (IC50 = 0.006 mu M) and good selectivity over HS27 fibroblast cell line. (C) 2010 Elsevier Ltd. All rights reserved.
Keywords
RANDOMIZED PHASE-III; METASTATIC MELANOMA; MALIGNANT-MELANOMA; DACARBAZINE; CHEMOTHERAPY; CISPLATIN; INTERLEUKIN-2; FOTEMUSTINE; EXPERIENCE; THERAPY; RANDOMIZED PHASE-III; METASTATIC MELANOMA; MALIGNANT-MELANOMA; DACARBAZINE; CHEMOTHERAPY; CISPLATIN; INTERLEUKIN-2; FOTEMUSTINE; EXPERIENCE; THERAPY; Aminoquinazolines; Synthesis; Antiproliferative activity; A375 human melanoma cell line; Selectivity
ISSN
0960-894X
URI
https://pubs.kist.re.kr/handle/201004/131011
DOI
10.1016/j.bmcl.2010.08.010
Appears in Collections:
KIST Article > 2010
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