Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines

J Lee, H Kim, H Yu, JY Chung, CH Oh, KH Yoo…

Index: Lee, Junghun; Kim, Hwan; Yu, Hana; Chung, Jae Yoon; Oh, Chang-Hyun; Yoo, Kyung Ho; Sim, Taebo; Hah, Jung-Mi Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 5 p. 1573 - 1577

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Citation Number: 22

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 ...