• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

合成的2'-羟基查尔酮类似物对前列腺素E2生成的抑制活性：合成与构效关系研究

Inhibitory activity of prostaglandin E2 production by the synthetic 2'-hydroxychalcone analogues: Synthesis and SAR study.

作者信息

Tran Thanh-Dao, Park Haeil, Kim Hyun Pyo, Ecker Gerhard F, Thai Khac-Minh

机构信息

Department of Pharmaceutical Chemistry, School of Pharmacy, University of Medicine and Pharmacy at Ho Chi Minh City, 41 Dinh Tien Hoang, Dist. 1, Ho Chi Minh City, Viet Nam.

出版信息

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1650-3. doi: 10.1016/j.bmcl.2009.02.001. Epub 2009 Feb 7.

DOI:10.1016/j.bmcl.2009.02.001
PMID:19233646
Abstract

A series of 2'-hydroxychalcones has been synthesized and screened for their in vitro inhibitory activities of cyclooxygenase-2 catalyzed prostaglandin production from lipopolysaccharide-treated RAW 264.7 cells. Structure-activity relationship study suggested that inhibitory activity against prostaglandin E(2) production was governed to a greater extent by the substituent on B ring of the chalcone, and most of the active compounds have at least two methoxy or benzyloxy groups on B ring. The relationship between chalcone structures and their PGE(2) inhibitory activities was also interpreted by docking study on cyclooxygenase-2.

摘要

合成了一系列2'-羟基查耳酮，并对其抑制脂多糖处理的RAW 264.7细胞中环氧化酶-2催化前列腺素生成的体外活性进行了筛选。构效关系研究表明，查耳酮B环上的取代基对前列腺素E(2)生成的抑制活性起更大作用，且大多数活性化合物在B环上至少有两个甲氧基或苄氧基。还通过对环氧化酶-2的对接研究解释了查耳酮结构与其PGE(2)抑制活性之间的关系。

相似文献

1
Inhibitory activity of prostaglandin E2 production by the synthetic 2'-hydroxychalcone analogues: Synthesis and SAR study.合成的2'-羟基查尔酮类似物对前列腺素E2生成的抑制活性：合成与构效关系研究
Bioorg Med Chem Lett. 2009 Mar 15;19(6):1650-3. doi: 10.1016/j.bmcl.2009.02.001. Epub 2009 Feb 7.
2
Design, synthesis and SAR study of hydroxychalcone inhibitors of human β-secretase (BACE1).设计、合成及对人β-分泌酶（BACE1）抑制剂类查尔酮的构效关系研究。
J Enzyme Inhib Med Chem. 2011 Oct;26(5):643-8. doi: 10.3109/14756366.2010.543420. Epub 2011 Jan 11.
3
Synthesis and evaluation of antiplatelet activity of trihydroxychalcone derivatives.三羟基查尔酮衍生物的合成及其抗血小板活性评估
Bioorg Med Chem Lett. 2005 Nov 15;15(22):5027-9. doi: 10.1016/j.bmcl.2005.08.039.
4
A SAR study on a series of synthetic lipophilic chalcones as inhibitor of transcription factor NF-κB.一种合成亲脂性查耳酮作为转录因子 NF-κB 抑制剂的 SAR 研究。
Eur J Med Chem. 2012 Aug;54:379-86. doi: 10.1016/j.ejmech.2012.05.019. Epub 2012 May 19.
5
Synthetic chalcones as potential anti-inflammatory and cancer chemopreventive agents.合成查耳酮作为潜在的抗炎和癌症化学预防剂。
Eur J Med Chem. 2005 Jan;40(1):103-12. doi: 10.1016/j.ejmech.2004.09.006.
6
Structural requirement of chalcones for the inhibitory activity of interleukin-5.查耳酮对白介素-5抑制活性的结构要求
Bioorg Med Chem. 2007 Jan 1;15(1):104-11. doi: 10.1016/j.bmc.2006.10.007. Epub 2006 Oct 10.
7
Inhibition of prostaglandin E(2) production by synthetic minor prenylated chalcones and flavonoids: synthesis, biological activity, crystal structure, and in silico evaluation.合成的小分子异戊烯基化查耳酮和黄酮类化合物对前列腺素E(2)生成的抑制作用：合成、生物活性、晶体结构及计算机模拟评估
Bioorg Med Chem Lett. 2014 Aug 15;24(16):3826-34. doi: 10.1016/j.bmcl.2014.06.061. Epub 2014 Jun 27.
8
Design, synthesis and in vitro antimalarial evaluation of triazole-linked chalcone and dienone hybrid compounds.三唑连接查尔酮和二烯酮杂合化合物的设计、合成及体外抗疟活性评价。
Bioorg Med Chem. 2010 Dec 1;18(23):8243-56. doi: 10.1016/j.bmc.2010.10.009. Epub 2010 Oct 31.
9
Synthesis and biological evaluation on novel analogs of 9-methylstreptimidone, an inhibitor of NF-kappaB.NF-κB抑制剂9-甲基链霉咪唑酮新型类似物的合成与生物学评价
Bioorg Med Chem Lett. 2009 Mar 15;19(6):1726-8. doi: 10.1016/j.bmcl.2009.01.107. Epub 2009 Feb 5.
10
Phenylsulphonyl urenyl chalcone derivatives as dual inhibitors of cyclo-oxygenase-2 and 5-lipoxygenase.苯磺酰脲基查尔酮衍生物作为环氧化酶-2和5-脂氧合酶的双重抑制剂
Life Sci. 2006 May 15;78(25):2911-8. doi: 10.1016/j.lfs.2005.11.017. Epub 2005 Dec 20.

引用本文的文献

1
Synthesis of Anti-Inflammatory Drugs' Chalcone Derivatives and a Study of Their Conformational Properties Through a Combination of Nuclear Magnetic Resonance Spectroscopy and Molecular Modeling.抗炎药物查尔酮衍生物的合成及其构象性质的研究——通过核磁共振光谱和分子建模相结合的方法
Pharmaceuticals (Basel). 2025 Jan 13;18(1):88. doi: 10.3390/ph18010088.
2
Chalcone Derivatives as Potential Inhibitors of P-Glycoprotein and NorA: An and Study.查尔酮衍生物作为 P-糖蛋白和 NorA 的潜在抑制剂：一项体外和体内研究。
Biomed Res Int. 2022 Mar 26;2022:9982453. doi: 10.1155/2022/9982453. eCollection 2022.
3
Characterization, molecular modeling and pharmacology of some 2́-hydroxychalcone derivatives as SARS-CoV-2 inhibitor.
某些2'-羟基查尔酮衍生物作为新型冠状病毒（SARS-CoV-2）抑制剂的表征、分子建模及药理学研究
Results Chem. 2022 Jan;4:100329. doi: 10.1016/j.rechem.2022.100329. Epub 2022 Mar 16.
4
Heterocyclization of polarized system: synthesis, antioxidant and anti-inflammatory 4-(pyridin-3-yl)-6-(thiophen-2-yl) pyrimidine-2-thiol derivatives.极化体系的杂环化：4-(吡啶-3-基)-6-(噻吩-2-基)嘧啶-2-硫醇衍生物的合成、抗氧化及抗炎作用
Chem Cent J. 2018 Jun 8;12(1):68. doi: 10.1186/s13065-018-0437-y.
5
Biocatalytic hydrogenation of the C=C bond in the enone unit of hydroxylated chalcones-process arising from cyanobacterial adaptations.生物催化氢化羟基查尔酮烯键：来自蓝藻适应的过程。
Appl Microbiol Biotechnol. 2018 Aug;102(16):7097-7111. doi: 10.1007/s00253-018-9109-z. Epub 2018 Jun 4.
6
Absence of genotoxic effects of the chalcone (E)-1-(2-hydroxyphenyl)-3-(4-methylphenyl)-prop-2-en-1-one) and its potential chemoprevention against DNA damage using in vitro and in vivo assays.查耳酮（E）-1-（2-羟基苯基）-3-（4-甲基苯基）-丙-2-烯-1-酮的遗传毒性作用缺失及其使用体外和体内试验对DNA损伤的潜在化学预防作用。
PLoS One. 2017 Feb 16;12(2):e0171224. doi: 10.1371/journal.pone.0171224. eCollection 2017.
7
Synthesis and Selective Cytotoxic Activities on Rhabdomyosarcoma and Noncancerous Cells of Some Heterocyclic Chalcones.某些杂环查耳酮对横纹肌肉瘤和非癌细胞的合成及选择性细胞毒性活性
Molecules. 2016 Mar 9;21(3):329. doi: 10.3390/molecules21030329.
8
Diverse Molecular Targets for Chalcones with Varied Bioactivities.具有多种生物活性的查耳酮的不同分子靶点。
Med Chem (Los Angeles). 2015 Aug;5(8):388-404. doi: 10.4172/2161-0444.1000291. Epub 2015 Aug 22.
9
Synthesis and antibacterial activity of some heterocyclic chalcone analogues alone and in combination with antibiotics.一些杂环查耳酮类似物的合成及单独和联合抗生素的抗菌活性。
Molecules. 2012 Jun 1;17(6):6684-96. doi: 10.3390/molecules17066684.
10
(E)-3-(4-Chloro-phen-yl)-1-(5-hy-droxy-2,2-dimethyl-2H-chromen-6-yl)prop-2-en-1-one.（E）-3-（4-氯苯基）-1-（5-羟基-2,2-二甲基-2H-色烯-6-基）丙-2-烯-1-酮
Acta Crystallogr Sect E Struct Rep Online. 2012 Feb 1;68(Pt 2):o278. doi: 10.1107/S1600536811055255. Epub 2012 Jan 7.