Yu, Hana Jung, Yunkyung Kim, Hwan Lee, Junghun Oh, Chang-Hyun Yoo, Kyung Ho Sim, Taebo Hah, Jung-Mi 2024-01-20T19:02:49Z 2024-01-20T19:02:49Z 2022-01-10 2010-06-15 0960-894X https://pubs.kist.re.kr/handle/201004/131327 The synthesis of a novel series of 1,4-dihydropyrazolo[4,3-d]imidazole phenyl derivatives 1a-b, 2a-v and their antiproliferative activities against A375P and WM3629 human melanoma cell line were described. Most compounds showed competitive antiproliferative activities to sorafenib, the reference standard. Among them, pyrazoloimidazole phenyl urea compounds 2a, 2d, 2g, 2i, 2t exhibited potent activities on WM3629 cell lines (IC50 = 0.56-0.86 mu M). Especially, 2t was found to be a potent and selective C-Raf inhibitor, showing a possibility as melanoma therapeutics. (C) 2010 Elsevier Ltd. All rights reserved. English Pergamon Press Ltd. B-RAF BRAF MUTATIONS MELANOMA DESIGN DISCOVERY PATHWAY CANCER CRAF 1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives: A novel type II Raf kinase inhibitors Article 10.1016/j.bmcl.2010.04.039 1 Bioorganic & Medicinal Chemistry Letters, v.20, no.12, pp.3805 - 3808 Bioorganic & Medicinal Chemistry Letters 20 12 3805 3808 scie scopus 000278208200078 2-s2.0-77954218062 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article B-RAF BRAF MUTATIONS MELANOMA DESIGN DISCOVERY PATHWAY CANCER CRAF 1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives Antiproliferative activity Melanoma cell line Selectivity