Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells
DC Field | Value | Language |
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dc.contributor.author | Kim, Mi-hyun | - |
dc.contributor.author | Kim, Minjung | - |
dc.contributor.author | Yu, Hana | - |
dc.contributor.author | Kim, Hwan | - |
dc.contributor.author | Yoo, Kyung Ho | - |
dc.contributor.author | Sim, Taebo | - |
dc.contributor.author | Hah, Jung-Mi | - |
dc.date.accessioned | 2021-06-23T11:04:34Z | - |
dc.date.available | 2021-06-23T11:04:34Z | - |
dc.date.created | 2021-01-21 | - |
dc.date.issued | 2011-03 | - |
dc.identifier.issn | 0968-0896 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/38204 | - |
dc.description.abstract | The synthesis of a novel series of N-(5-amino-1-(4-methoxybenzyl)-1H-pyrazol-4-yl amide derivatives 6a-o, 7a-s and their antiproliferative activities against A375P melanoma cell line were described. Most compounds showed competitive antiproliferative activities to sorafenib, the reference standard. Among them, N-(5-amino-1-(4-methoxybenzyl)-1H-pyrazol-4-yl)-5-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-2-methylbenzamide 7c exhibited potent activities (GI(50) = 0.27 mu M). Especially, 7c was found to be a potent and selective B-Raf V600E and C-Raf inhibitor (IC50 = 0.26 mu M, IC50 = 0.11 mu M, respectively), showing a possibility as melanoma therapeutics. (C) 2011 Elsevier Ltd. All rights reserved. | - |
dc.language | 영어 | - |
dc.language.iso | en | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.title | Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Hah, Jung-Mi | - |
dc.identifier.doi | 10.1016/j.bmc.2011.01.067 | - |
dc.identifier.scopusid | 2-s2.0-79952453681 | - |
dc.identifier.wosid | 000288196900008 | - |
dc.identifier.bibliographicCitation | BIOORGANIC & MEDICINAL CHEMISTRY, v.19, no.6, pp.1915 - 1923 | - |
dc.relation.isPartOf | BIOORGANIC & MEDICINAL CHEMISTRY | - |
dc.citation.title | BIOORGANIC & MEDICINAL CHEMISTRY | - |
dc.citation.volume | 19 | - |
dc.citation.number | 6 | - |
dc.citation.startPage | 1915 | - |
dc.citation.endPage | 1923 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.isOpenAccess | N | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Biochemistry & Molecular Biology | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Biochemistry & Molecular Biology | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
dc.subject.keywordPlus | BRAF | - |
dc.subject.keywordPlus | MUTATIONS | - |
dc.subject.keywordPlus | CRAF | - |
dc.subject.keywordAuthor | Aminopyrazole amide | - |
dc.subject.keywordAuthor | Antiproliferative activity | - |
dc.subject.keywordAuthor | Melanoma cell line | - |
dc.subject.keywordAuthor | Kinase inhibitor | - |
dc.subject.keywordAuthor | Kinase selectivity | - |
dc.identifier.url | https://www.sciencedirect.com/science/article/pii/S0968089611000964?via%3Dihub | - |
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