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 μM, respectively) and turned out to be a selective and potent CRAF inhibitor.
| Original language | English |
|---|---|
| Pages (from-to) | 1573-1577 |
| Number of pages | 5 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 20 |
| Issue number | 5 |
| DOIs | |
| Publication status | Published - 2010 Mar 1 |
Keywords
- Antiproliferative activity
- BRAF
- CRAF
- Melanoma cell line
- Pyrimidin-4-yl-1H-imidazol-2-yl derivatives
- Selectivity
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry
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Cite this
Lee, J., Kim, H., Yu, H., Chung, J. Y., Oh, C. H., Yoo, K. H., Sim, T., & Hah, J. M. (2010). Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines. Bioorganic and Medicinal Chemistry Letters, 20(5), 1573-1577. https://doi.org/10.1016/j.bmcl.2010.01.064