Discovery and Initial SAR of Pyrimidin-4-yl-1H-imidazole derivatives with Antiproliferative activity against Melanoma cell lines
- Discovery and Initial SAR of Pyrimidin-4-yl-1H-imidazole derivatives with Antiproliferative activity against Melanoma cell lines
- 이정헌; 김환; 유하나; 정재윤; 오창현; 유경호; 심태보; 하정미
- Pyrimidin-4-yl-1H-imidazol-2-yl; derivatives; Antiproliferative activity; Melanoma cell line; BRAF; CRAF; Selectivity
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 20, NO 5, 1573-1577
- 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.
- Appears in Collections:
- KIST Publication > Article
- Files in This Item:
There are no files associated with this item.
- RIS (EndNote)
- XLS (Excel)
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.