Lee, Junghun Kim, Hwan Yu, Hana Chung, Jae Yoon Oh, Chang-Hyun Yoo, Kyung Ho Sim, Taebo Hah, Jung-Mi 2024-01-20T19:34:22Z 2024-01-20T19:34:22Z 2021-09-01 2010-03-01 0960-894X https://pubs.kist.re.kr/handle/201004/131650 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. English Pergamon Press Ltd. MALIGNANT-MELANOMA BRAF KINASE INHIBITOR MUTATIONS CRAF SORAFENIB CANCER RAF ERK Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines Article 10.1016/j.bmcl.2010.01.064 1 Bioorganic & Medicinal Chemistry Letters, v.20, no.5, pp.1573 - 1577 Bioorganic & Medicinal Chemistry Letters 20 5 1573 1577 scie scopus 000274714600023 2-s2.0-76649090272 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article MALIGNANT-MELANOMA BRAF KINASE INHIBITOR MUTATIONS CRAF SORAFENIB CANCER RAF ERK Pyrimidin-4-yl-1H-imidazol-2-yl derivatives Antiproliferative activity Melanoma cell line BRAF CRAF Selectivity