• 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

用于基于片段的碳酸酐酶抑制剂药物发现的多样化取代磺胺：合成和抑制谱。

Diversely substituted sulfamides for fragment-based drug discovery of carbonic anhydrase inhibitors: synthesis and inhibitory profile.

机构信息

Institute of Chemistry, Saint Petersburg State University, Saint Petersburg, Russia.

Neurofarba Department, Universita Degli Studi di Firenze, Florence, Italy.

出版信息

J Enzyme Inhib Med Chem. 2022 Dec;37(1):857-865. doi: 10.1080/14756366.2022.2051023.

DOI:10.1080/14756366.2022.2051023
PMID:35296197
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8933014/
Abstract

A series of sulfamide fragments has been synthesised and investigated for human carbonic anhydrase inhibition. One of the fragments showing greater selectivity for cancer-related isoforms CA IX and XII was co-crystalized with CA II showing significant potential for fragment periphery evolution fragment growth and linking. These opportunities will be identified in the future the screening of this fragment structure for co-operative carbonic anhydrase binding with other structurally diverse fragments.[Figure: see text].

摘要

已经合成了一系列磺胺片段，并对其进行了人类碳酸酐酶抑制活性的研究。其中一个片段对与癌症相关的同工酶 CAIX 和 CA XII 表现出更高的选择性，与 CA II 共结晶显示出了对片段外围进化、片段生长和连接具有显著潜力。未来将确定这些机会，并对该片段结构进行筛选，以寻找与其他结构多样的片段的协同碳酸酐酶结合。[图：见正文]。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eac2/8933014/441019794feb/IENZ_A_2051023_F0003_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eac2/8933014/79a5009718e4/IENZ_A_2051023_UF0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eac2/8933014/8ae62485d7f1/IENZ_A_2051023_F0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eac2/8933014/fb05efbcabb4/IENZ_A_2051023_F0002_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eac2/8933014/24a51a959059/IENZ_A_2051023_SCH0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eac2/8933014/804bed556a2f/IENZ_A_2051023_SCH0002_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eac2/8933014/441019794feb/IENZ_A_2051023_F0003_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eac2/8933014/79a5009718e4/IENZ_A_2051023_UF0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eac2/8933014/8ae62485d7f1/IENZ_A_2051023_F0001_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eac2/8933014/fb05efbcabb4/IENZ_A_2051023_F0002_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eac2/8933014/24a51a959059/IENZ_A_2051023_SCH0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eac2/8933014/804bed556a2f/IENZ_A_2051023_SCH0002_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eac2/8933014/441019794feb/IENZ_A_2051023_F0003_C.jpg

相似文献

1
Diversely substituted sulfamides for fragment-based drug discovery of carbonic anhydrase inhibitors: synthesis and inhibitory profile.用于基于片段的碳酸酐酶抑制剂药物发现的多样化取代磺胺：合成和抑制谱。
J Enzyme Inhib Med Chem. 2022 Dec;37(1):857-865. doi: 10.1080/14756366.2022.2051023.
2
Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity.含哌嗪基脲部分的磺胺类药物的合成及其对碳酸酐酶I、II、IX和XII的抑制活性。
Bioorg Med Chem Lett. 2015 Sep 15;25(18):3850-3. doi: 10.1016/j.bmcl.2015.07.060. Epub 2015 Jul 26.
3
Synthesis of a new series of N⁴-substituted 4-(2-aminoethyl)benzenesulfonamides and their inhibitory effect on human carbonic anhydrase cytosolic isozymes I and II and transmembrane tumor-associated isozymes IX and XII.合成一系列新型的 N⁴-取代的 4-(2-氨乙基)苯磺酰胺及其对人碳酸酐酶胞质同工酶 I 和 II 以及跨膜肿瘤相关同工酶 IX 和 XII 的抑制作用。
Eur J Med Chem. 2014 Sep 12;84:59-67. doi: 10.1016/j.ejmech.2014.06.074. Epub 2014 Jul 5.
4
S-substituted 2-mercaptoquinazolin-4(3H)-one and 4-ethylbenzensulfonamides act as potent and selective human carbonic anhydrase IX and XII inhibitors.S-取代的 2-巯基喹唑啉-4(3H)-酮和 4-乙基苯磺酰胺类化合物可作为强效和选择性的人碳酸酐酶 IX 和 XII 抑制剂。
J Enzyme Inhib Med Chem. 2020 Dec;35(1):733-743. doi: 10.1080/14756366.2020.1742117.
5
Carbonic anhydrase inhibitors. Synthesis of a novel series of 5-substituted 2,4-dichlorobenzenesulfonamides and their inhibition of human cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII.碳酸酐酶抑制剂。新型5-取代2,4-二氯苯磺酰胺系列的合成及其对人胞质同工酶I和II以及跨膜肿瘤相关同工酶IX和XII的抑制作用。
Eur J Med Chem. 2014 Jul 23;82:47-55. doi: 10.1016/j.ejmech.2014.05.039. Epub 2014 May 13.
6
Design, synthesis and human carbonic anhydrase I, II, IX and XII inhibitory properties of 1,3-thiazole sulfonamides.1,3-噻唑磺酰胺的设计、合成及其对人碳酸酐酶I、II、IX和XII的抑制特性
Bioorg Med Chem Lett. 2022 Mar 1;59:128581. doi: 10.1016/j.bmcl.2022.128581. Epub 2022 Jan 20.
7
Discovery of curcumin inspired sulfonamide derivatives as a new class of carbonic anhydrase isoforms I, II, IX, and XII inhibitors.姜黄素启发下的磺酰胺衍生物作为一类新型碳酸酐酶同工酶I、II、IX和XII抑制剂的发现。
J Enzyme Inhib Med Chem. 2017 Dec;32(1):1274-1281. doi: 10.1080/14756366.2017.1380638.
8
Carbonic anhydrase inhibitors. Synthesis of heterocyclic 4-substituted pyridine-3-sulfonamide derivatives and their inhibition of the human cytosolic isozymes I and II and transmembrane tumor-associated isozymes IX and XII.碳酸酐酶抑制剂。杂环 4-取代吡啶-3-磺酰胺衍生物的合成及其对人胞质同工酶 I 和 II 以及跨膜肿瘤相关同工酶 IX 和 XII 的抑制作用。
Eur J Med Chem. 2013 Nov;69:701-10. doi: 10.1016/j.ejmech.2013.09.027. Epub 2013 Sep 20.
9
Carbonic anhydrase inhibitors: Synthesis, molecular docking, cytotoxic and inhibition of the human carbonic anhydrase isoforms I, II, IX, XII with novel benzenesulfonamides incorporating pyrrole, pyrrolopyrimidine and fused pyrrolopyrimidine moieties.碳酸酐酶抑制剂：新型苯磺酰胺类化合物的合成、分子对接、细胞毒性及对人碳酸酐酶同工酶 I、II、IX、XII 的抑制作用，其中包含吡咯、吡咯嘧啶和稠合吡咯嘧啶部分。
Bioorg Med Chem. 2014 Jul 15;22(14):3684-95. doi: 10.1016/j.bmc.2014.05.009. Epub 2014 May 14.
10
Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors.合成、生物和分子动力学研究一系列三唑并嘧啶/三唑基苯磺酰胺作为新型碳酸酐酶抑制剂。
Eur J Med Chem. 2020 Jan 1;185:111843. doi: 10.1016/j.ejmech.2019.111843. Epub 2019 Nov 2.

引用本文的文献

1
Melanin-Binding-Based Discovery of Topically Instilled Carbonic Anhydrase Inhibitors for Targeted Delivery and Prolonged Action in the Eye.基于黑色素结合的局部滴注碳酸酐酶抑制剂的发现，用于眼部的靶向递送和长效作用。
Mol Pharm. 2025 Feb 3;22(2):721-732. doi: 10.1021/acs.molpharmaceut.4c00694. Epub 2025 Jan 9.

本文引用的文献

1
The impact of tumour pH on cancer progression: strategies for clinical intervention.肿瘤pH值对癌症进展的影响：临床干预策略
Explor Target Antitumor Ther. 2020;1(2):71-100. doi: 10.37349/etat.2020.00005. Epub 2020 Apr 28.
2
Carbonic Anhydrase Inhibitors and Epilepsy: State of the Art and Future Perspectives.碳酸酐酶抑制剂与癫痫：现状与未来展望。
Molecules. 2021 Oct 22;26(21):6380. doi: 10.3390/molecules26216380.
3
Selective Inhibition of Carbonic Anhydrases by Carvacrol and Thymol Could Impair Biofilm Production and the Release of Outer Membrane Vesicles.
香芹酚和百里香酚对碳酸酐酶的选择性抑制作用可能会损害生物膜的产生和外膜囊泡的释放。
Int J Mol Sci. 2021 Oct 27;22(21):11583. doi: 10.3390/ijms222111583.
4
Application of Fragment-Based Drug Discovery to Versatile Targets.基于片段的药物发现技术在多种靶点中的应用。
Front Mol Biosci. 2020 Aug 5;7:180. doi: 10.3389/fmolb.2020.00180. eCollection 2020.
5
Antibacterial carbonic anhydrase inhibitors: an update on the recent literature.抗菌碳酸酐酶抑制剂：最新文献综述。
Expert Opin Ther Pat. 2020 Dec;30(12):963-982. doi: 10.1080/13543776.2020.1811853. Epub 2020 Sep 3.
6
The Effect of Substituted Benzene-Sulfonamides and Clinically Licensed Drugs on the Catalytic Activity of CynT2, a Carbonic Anhydrase Crucial for Life Cycle.取代苯磺酰胺类化合物和临床许可药物对生命循环中关键的碳酸酐酶 CynT2 的催化活性的影响。
Int J Mol Sci. 2020 Jun 11;21(11):4175. doi: 10.3390/ijms21114175.
7
Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action.通过三尾法设计的人碳酸酐酶的磺胺抑制剂：改善配体/同工型匹配和作用选择性。
J Med Chem. 2020 Jul 9;63(13):7422-7444. doi: 10.1021/acs.jmedchem.0c00733. Epub 2020 Jun 22.
8
Screening of benzenesulfonamide in combination with chemically diverse fragments against carbonic anhydrase by differential scanning fluorimetry.用差示扫描荧光法筛选苯磺酰胺与化学多样性片段的组合对碳酸酐酶的抑制作用。
J Enzyme Inhib Med Chem. 2020 Dec;35(1):306-310. doi: 10.1080/14756366.2019.1698562.
9
Polypharmacology of epacadostat: a potent and selective inhibitor of the tumor associated carbonic anhydrases IX and XII.依帕司他的多药理学特性：一种有效的、肿瘤相关碳酸酐酶 IX 和 XII 的选择性抑制剂。
Chem Commun (Camb). 2019 May 14;55(40):5720-5723. doi: 10.1039/c8cc09568j.
10
Acetazolamide Therapy in Patients with Heart Failure: A Meta-Analysis.心力衰竭患者的乙酰唑胺治疗：一项荟萃分析。
J Clin Med. 2019 Mar 12;8(3):349. doi: 10.3390/jcm8030349.