Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 하정미 | - |
dc.date.accessioned | 2023-08-23T01:15:38Z | - |
dc.date.available | 2023-08-23T01:15:38Z | - |
dc.date.issued | 2011-11 | - |
dc.identifier.citation | BIOORGANIC & MEDICINAL CHEMISTRY, v. 19, NO. 22, Page. 6760-6767 | - |
dc.identifier.issn | 0968-0896;1464-3391 | - |
dc.identifier.uri | https://www.sciencedirect.com/science/article/pii/S0968089611007772?via%3Dihub | en_US |
dc.identifier.uri | https://repository.hanyang.ac.kr/handle/20.500.11754/186138 | - |
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 | en | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.subject | Dihydropyrazolodiazepinone | - |
dc.subject | Antiproliferative activity | - |
dc.subject | Cancer cell line | - |
dc.subject | Kinase inhibitor | - |
dc.subject | Kinase selectivity | - |
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.relation.no | 22 | - |
dc.relation.volume | 19 | - |
dc.identifier.doi | 10.1016/j.bmc.2011.09.042 | - |
dc.relation.page | 6760-6767 | - |
dc.relation.journal | BIOORGANIC & MEDICINAL CHEMISTRY | - |
dc.contributor.googleauthor | Kim, Hyangmi | - |
dc.contributor.googleauthor | Kim, Minjung | - |
dc.contributor.googleauthor | Lee, Junghun | - |
dc.contributor.googleauthor | Yu, Hana | - |
dc.contributor.googleauthor | Hah, Jung-Mi | - |
dc.sector.campus | E | - |
dc.sector.daehak | 약학대학 | - |
dc.sector.department | 약학과 | - |
dc.identifier.pid | jhah | - |
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