Synthesis of 8-Amino(acetamido)quinoline Derivatives and Their Antiproliferative Activities against Melanoma Cell Lines

Title
Synthesis of 8-Amino(acetamido)quinoline Derivatives and Their Antiproliferative Activities against Melanoma Cell Lines
Authors
유경호고은정이상기
Keywords
8-Amino(acetamido)quinolines; Antiproliferative Activities; Melanoma Cell Lines
Issue Date
2013-08
Publisher
44th World Chemistry Congress
Abstract
Melanoma is the most aggressive type of skin cancer. It is considered as a malignant tumor of melanocytes. Patients with advanced melanoma have a median survival time of less than one year, and the estimated 5-year survival rate is less than 15%.[1,2] A number of reports have recently reported diarylamides and diarylureas with potential antiproliferative activities against melanoma cell lines.[3] In this work, a new series of 8-amino(acetamido)quinolines were evaluated for antiproliferative activities against ten human melanoma cell lines, in silico studies, and ERK kinases inhibitory activities. Compounds 1l, 2l, 3c, and 4c showed the highest potency against A375P cell line with IC50 values in sub-micromolar scale. In addition, compounds 1l, 2a, and 2l demonstrated the highest potencies over NCI-9 melanoma cell line panel. Of special interest, compounds 1l and 2l exerted 2-digit nanomolar IC50 values over four and five cell lines, respectively. Compounds 2l and 4c showed significant and dose-dependent ERK kinase inhibitory activity. This study led to discovery of two lead compounds for future development of antiproliferative agents targeting ERK pathway for treatment of melanoma, 1l and 2l, with amide linker and 2,3-dihydrobenzo[b][1,4]dioxine terminal moiety.
URI
http://pubs.kist.re.kr/handle/201004/46631
Appears in Collections:
KIST Publication > Conference Paper
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