Figshare最新文献

筛选
英文 中文
Design, Synthesis,nand Biological Activity of New <i>N</i>‑(Phenylmethyl)-benzoxazol-2-thionesnas MacrophagenMigration Inhibitory Factor (MIF) Antagonists: Efficacies in ExperimentalnPulmonary Hypertension 新型(苯基甲基)-苯并恶唑-2-硫酮类巨噬细胞迁移抑制因子(MIF)拮抗剂的设计、合成、生物活性及对实验性肺动脉高压的影响
Figshare Pub Date : 2018-03-19 DOI: 10.1021/acs.jmedchem.7b01312.s001
Morane Le Hiress (4975352), Bernardin Akagah (4975349), Guillaume Bernadat (1525456), Ly Tu (4975355), Raphaël Thuillet (4975346), Alice Huertas (4975367), Carole Phan (4975358), Elie Fadel (471021), Gérald Simonneau (3727672), Marc Humbert (23466), Gaël Jalce (4975361), Christophe Guignabert (4975364)
{"title":"Design, Synthesis,nand Biological Activity of New &lt;i&gt;N&lt;/i&gt;‑(Phenylmethyl)-benzoxazol-2-thionesnas MacrophagenMigration Inhibitory Factor (MIF) Antagonists: Efficacies in ExperimentalnPulmonary Hypertension","authors":"Morane Le Hiress (4975352), Bernardin Akagah (4975349), Guillaume Bernadat (1525456), Ly Tu (4975355), Raphaël Thuillet (4975346), Alice Huertas (4975367), Carole Phan (4975358), Elie Fadel (471021), Gérald Simonneau (3727672), Marc Humbert (23466), Gaël Jalce (4975361), Christophe Guignabert (4975364)","doi":"10.1021/acs.jmedchem.7b01312.s001","DOIUrl":"https://doi.org/10.1021/acs.jmedchem.7b01312.s001","url":null,"abstract":"Macrophagenmigration inhibitory factor (MIF) is a key pleiotropicnmediator and a promising therapeutic target in cancer as well as innseveral inflammatory and cardiovascular diseases including pulmonarynarterial hypertension (PAH). Here, a novel series of &lt;i&gt;N&lt;/i&gt;-(phenylmethyl)-benzoxazol-2-thiones &lt;b&gt;5&lt;/b&gt;–&lt;b&gt;32&lt;/b&gt; designed to target the MIF tautomerase active site wasnsynthesized and evaluated for its effects on cell survival. Investigationnof structure–activity relationship (SAR) particularly at then5-position of the benzoxazole core led to the identification of &lt;b&gt;31&lt;/b&gt; that potently inhibits cell survival in DU-145 prostatencancer cells and pulmonary endothelial cells derived from patientsnwith idiopathic PAH (iPAH-ECs), two cell lines for which survivalnis MIF-dependent. Molecular docking studies helped to interpret initialnSAR related to MIF tautomerase inhibition and propose preferred bindingnmode for &lt;b&gt;31&lt;/b&gt; within the MIF tautomerase active site. Interestingly,ndaily treatment with &lt;b&gt;31&lt;/b&gt; started 2 weeks after a subcutaneousnmonocrotaline injection regressed established pulmonary hypertensionnin rats.","PeriodicalId":522888,"journal":{"name":"Figshare","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147905568","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
相关产品
×
本文献相关产品
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信
小红书