Synthesis of 8-Amino(acetamido)quinoline Derivatives and Their Antiproliferative Activities against Melanoma Cell Lines
- Synthesis of 8-Amino(acetamido)quinoline Derivatives and Their Antiproliferative Activities against Melanoma Cell Lines
- 유경호; 고은정; 이상기
- 8-Amino(acetamido)quinolines; Antiproliferative Activities; Melanoma Cell Lines
- Issue Date
- 44th World Chemistry Congress
- 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. 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.
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