Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Kim, Hyangmi | - |
dc.contributor.author | Kim, Minjung | - |
dc.contributor.author | Lee, Junghun | - |
dc.contributor.author | Yu, Hana | - |
dc.contributor.author | Hah, Jung-Mi | - |
dc.date.accessioned | 2021-06-23T10:05:12Z | - |
dc.date.available | 2021-06-23T10:05:12Z | - |
dc.date.created | 2021-01-21 | - |
dc.date.issued | 2011-11 | - |
dc.identifier.issn | 0968-0896 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/36407 | - |
dc.description.abstract | Recently, we have reported the syntheses and antiproliferative activities of N-(5-amino-1-(4-methoxybenzyl)-1H-pyrazol-4-yl amide derivatives on melanoma cells. As a continuous work for antiproliferative agents in melanoma, here we report the synthesis of conformationally rigid analogs, phenyl-6,8-dihydropyrazolo[3,4-b][1,4] diazepin-7(1H)-one derivatives7a-g, 8a-o and their antiproliferative activities against A375P melanoma cell line and U937 hematopoietic cell line. Most compounds showed competitive antiproliferative activities to sorafenib, the reference standard. Among them, N-(3-(1-benzyl-7-oxo-1,6, 7,8-tetrahydropyrazolo[3,4-b][1,4]diazepin-5-yl)phenyl)-4-chloro-3-(trifluoro methyl)benzamide-amino1-(4-methoxybenzyl)-1H-pyrazol-4-yl)-5-(3-(4-chloro-3-(trifluoromethyl) phenyl) ureido)-2-methylbenzamide (7b) exhibited potent activities (GI(50) = 0.43 mu M and 0.06 mu M) on both cell lines. It has been further confirmed to be a potent and selective Raf kinases inhibitor and also mild inhibitor of PI3K alpha. (C) 2011 Elsevier Ltd. All rights reserved. | - |
dc.language | 영어 | - |
dc.language.iso | en | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.title | Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Hah, Jung-Mi | - |
dc.identifier.doi | 10.1016/j.bmc.2011.09.042 | - |
dc.identifier.scopusid | 2-s2.0-80054974235 | - |
dc.identifier.wosid | 000296535900026 | - |
dc.identifier.bibliographicCitation | BIOORGANIC & MEDICINAL CHEMISTRY, v.19, no.22, pp.6760 - 6767 | - |
dc.relation.isPartOf | BIOORGANIC & MEDICINAL CHEMISTRY | - |
dc.citation.title | BIOORGANIC & MEDICINAL CHEMISTRY | - |
dc.citation.volume | 19 | - |
dc.citation.number | 22 | - |
dc.citation.startPage | 6760 | - |
dc.citation.endPage | 6767 | - |
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 | KINASE INHIBITORS | - |
dc.subject.keywordPlus | PATHWAY | - |
dc.subject.keywordPlus | BRAF | - |
dc.subject.keywordPlus | PI3K/PTEN/AKT/MTOR | - |
dc.subject.keywordPlus | RAS/RAF/MEK/ERK | - |
dc.subject.keywordPlus | DISCOVERY | - |
dc.subject.keywordPlus | MUTATIONS | - |
dc.subject.keywordPlus | LEUKEMIA | - |
dc.subject.keywordPlus | MELANOMA | - |
dc.subject.keywordPlus | TARGET | - |
dc.subject.keywordAuthor | Dihydropyrazolodiazepinone | - |
dc.subject.keywordAuthor | Antiproliferative activity | - |
dc.subject.keywordAuthor | Cancer cell line | - |
dc.subject.keywordAuthor | Kinase inhibitor | - |
dc.subject.keywordAuthor | Kinase selectivity | - |
dc.identifier.url | https://www.sciencedirect.com/science/article/pii/S0968089611007772?via%3Dihub | - |
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.
55 Hanyangdeahak-ro, Sangnok-gu, Ansan, Gyeonggi-do, 15588, Korea+82-31-400-4269 sweetbrain@hanyang.ac.kr
COPYRIGHT © 2021 HANYANG UNIVERSITY. ALL RIGHTS RESERVED.
Certain data included herein are derived from the © Web of Science of Clarivate Analytics. All rights reserved.
You may not copy or re-distribute this material in whole or in part without the prior written consent of Clarivate Analytics.