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1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives: A novel type II Raf kinase inhibitors
- Authors
- Yu, Hana; Jung, Yunkyung; Kim, Hwan; Lee, Junghun; Oh, Chang-Hyun; Yoo, Kyung Ho; Sim, Taebo; Hah, Jung-Mi
- Issue Date
- Jun-2010
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- 1,4-Dihydropyrazolo[4,3-d]imidazole; phenyl derivatives; Antiproliferative activity; Melanoma cell line; Selectivity
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.20, no.12, pp.3805 - 3808
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 20
- Number
- 12
- Start Page
- 3805
- End Page
- 3808
- ISSN
- 0960-894X
- Abstract
- 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.
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Related Researcher
- Hah, Jung Mi
- COLLEGE OF PHARMACY (DEPARTMENT OF PHARMACY)