Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines
- Authors
- Lee, Junghun; Kim, Hwan; Yu, Hana; Chung, Jae Yoon; Oh, Chang-Hyun; Yoo, Kyung Ho; Sim, Taebo; Hah, Jung-Mi
- Issue Date
- Mar-2010
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Pyrimidin-4-yl-1H-imidazol-2-yl derivatives; Antiproliferative activity; Melanoma cell line; BRAF; CRAF; Selectivity
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.20, no.5, pp.1573 - 1577
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 20
- Number
- 5
- Start Page
- 1573
- End Page
- 1577
- URI
- https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/39934
- DOI
- 10.1016/j.bmcl.2010.01.064
- ISSN
- 0960-894X
- Abstract
- The synthesis of a novel series of pyrimidin-4-yl-1H-imidazol-2-yl derivatives 7, 8, 9 and their antiproliferative activities against A375P human melanoma cell line and WM3629 cell line were described. Most compounds showed superior antiproliferative activities compared to Sorafenib, the well-known RAF inhibitor. Among them, 7a exhibited potent activities on both cell lines (IC50 = 0.62 and 4.49 mu M, respectively) and turned out to be a selective and potent CRAF inhibitor. (C) 2010 Elsevier Ltd. All rights reserved.
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