• 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

苯并噻唑-2-硫醇衍生物的合成、构效关系及初步抗肿瘤活性评价

Synthesis, structure-activity relationships and preliminary antitumor evaluation of benzothiazole-2-thiol derivatives as novel apoptosis inducers.

机构信息

State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Sichuan 610041, China.

出版信息

Bioorg Med Chem Lett. 2011 Feb 15;21(4):1097-101. doi: 10.1016/j.bmcl.2010.12.124. Epub 2010 Dec 31.

DOI:10.1016/j.bmcl.2010.12.124
PMID:21262571
Abstract

A series of novel benzothiazole-2-thiol derivatives were synthesized, and their anti-proliferative activities on HepG2 and MCF-7 cells were investigated. Most compounds had inhibitory effects on cell growth, and some of them were more effective than cisplatin. Compounds 6m and 6t displayed good inhibitory activities against a panel of different types of human cancer cell lines, with IC(50) values in the low micromolar range. Further biological evaluation indicated that 6m induced apoptosis in HepG2 cancer cells. Structure-activity relationships were also proposed.

摘要

合成了一系列新型苯并噻唑-2-硫醇衍生物，并研究了它们对 HepG2 和 MCF-7 细胞的抗增殖活性。大多数化合物对细胞生长有抑制作用，其中一些比顺铂更有效。化合物 6m 和 6t 对一系列不同类型的人癌细胞系表现出良好的抑制活性，IC50值在低微摩尔范围内。进一步的生物学评价表明，6m 诱导 HepG2 癌细胞凋亡。还提出了构效关系。

相似文献

1
Synthesis, structure-activity relationships and preliminary antitumor evaluation of benzothiazole-2-thiol derivatives as novel apoptosis inducers.苯并噻唑-2-硫醇衍生物的合成、构效关系及初步抗肿瘤活性评价
Bioorg Med Chem Lett. 2011 Feb 15;21(4):1097-101. doi: 10.1016/j.bmcl.2010.12.124. Epub 2010 Dec 31.
2
Synthesis and biological evaluation of mercapto triazolo-benzothiadiazine linked aminobenzothiazoles as potential anticancer agents.巯基三唑并苯并噻二嗪连接的氨基苯并噻唑作为潜在抗癌剂的合成及生物学评价
Chem Biol Drug Des. 2009 Jun;73(6):687-93. doi: 10.1111/j.1747-0285.2009.00815.x.
3
[Synthesis and antitumor activity of 5-substituted-2-(pyridyl)benzothiazole compounds].5-取代-2-(吡啶基)苯并噻唑化合物的合成及其抗肿瘤活性
Yao Xue Xue Bao. 2013 Jan;48(1):83-8.
4
Antitumor benzothiazoles. 26.(1) 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (GW 610, NSC 721648), a simple fluorinated 2-arylbenzothiazole, shows potent and selective inhibitory activity against lung, colon, and breast cancer cell lines.抗肿瘤苯并噻唑类化合物。26.（1）2-（3,4-二甲氧基苯基）-5-氟苯并噻唑（GW 610，NSC 721648），一种简单的氟化2-芳基苯并噻唑，对肺癌、结肠癌和乳腺癌细胞系显示出强效且选择性的抑制活性。
J Med Chem. 2006 Jan 12;49(1):179-85. doi: 10.1021/jm050942k.
5
Synthesis, characterization and biological evaluation of some thiourea derivatives bearing benzothiazole moiety as potential antimicrobial and anticancer agents.合成、表征及含苯并噻唑基的硫脲衍生物的生物评价作为潜在的抗菌和抗癌药物。
Eur J Med Chem. 2010 Apr;45(4):1323-31. doi: 10.1016/j.ejmech.2009.12.016. Epub 2009 Dec 16.
6
Novel cyano- and amidinobenzothiazole derivatives: synthesis, antitumor evaluation, and X-ray and quantitative structure-activity relationship (QSAR) analysis.新型氰基和脒基苯并噻唑衍生物：合成、抗肿瘤评估以及X射线和定量构效关系（QSAR）分析
J Med Chem. 2009 Mar 26;52(6):1744-56. doi: 10.1021/jm801566q.
7
Synthesis, anticancer activity and docking of some substituted benzothiazoles as tyrosine kinase inhibitors.合成、抗癌活性和一些取代苯并噻唑作为酪氨酸激酶抑制剂的对接。
J Mol Graph Model. 2010 Aug 24;29(1):32-7. doi: 10.1016/j.jmgm.2010.04.003. Epub 2010 Apr 24.
8
Synthesis of some N-[4-(benzothiazole-2yl) phenyl]-2-aryloxyacetamide derivatives and their anticancer activities.合成一些 N-[4-(苯并噻唑-2-基)苯基]-2-芳氧基乙酰胺衍生物及其抗癌活性。
J Enzyme Inhib Med Chem. 2012 Aug;27(4):515-20. doi: 10.3109/14756366.2011.599030. Epub 2011 Aug 8.
9
Synthesis and in vitro antitumor activity of new series of benzothiazole and pyrimido[2,1-b]benzothiazole derivatives.新型苯并噻唑和嘧啶并[2,1 - b]苯并噻唑衍生物系列的合成及其体外抗肿瘤活性
Eur J Med Chem. 2014 Oct 6;85:576-92. doi: 10.1016/j.ejmech.2014.07.097. Epub 2014 Jul 29.
10
Synthesis and biological evaluation of novel benzothiazole-2-thiol derivatives as potential anticancer agents.新型苯并噻唑-2-硫醇衍生物的合成及生物评价作为潜在的抗癌剂。
Molecules. 2012 Mar 30;17(4):3933-44. doi: 10.3390/molecules17043933.

引用本文的文献

1
Synthesis, Molecular Docking, and Antimicrobial Evaluation of 2-(Substituted Amino)-N-(6-Substituted-1,3-Benzothiazol-2yl) Acetamide.2-（取代氨基）-N-（6-取代-1,3-苯并噻唑-2-基）乙酰胺的合成、分子对接及抗菌活性评价
Curr Drug Discov Technol. 2025;22(3):e200624231065. doi: 10.2174/0115701638299377240604112400.
2
Design, synthesis, molecular modelling and biological evaluation of novel 6-amino-5-cyano-2-thiopyrimidine derivatives as potent anticancer agents against leukemia and apoptotic inducers.新型 6-氨基-5-氰基-2-嘧啶硫酮衍生物的设计、合成、分子模拟及作为白血病潜在抗癌剂和凋亡诱导剂的生物学评价。
J Enzyme Inhib Med Chem. 2024 Dec;39(1):2304625. doi: 10.1080/14756366.2024.2304625. Epub 2024 Feb 13.
3
Design, synthesis, studies, and biological evaluation of novel pyrimidine-5-carbonitrile derivatives as potential anti-proliferative agents, VEGFR-2 inhibitors and apoptotic inducers.
新型嘧啶-5-腈衍生物作为潜在抗增殖剂、VEGFR-2抑制剂和凋亡诱导剂的设计、合成、研究及生物学评价
RSC Adv. 2023 Jul 24;13(32):22122-22147. doi: 10.1039/d3ra04182d. eCollection 2023 Jul 19.
4
A novel benzothiazole derivative induces apoptosis via the mitochondrial intrinsic pathway producing antitumor activity in colorectal cancer.一种新型苯并噻唑衍生物通过线粒体内在途径诱导细胞凋亡，从而在结直肠癌中产生抗肿瘤活性。
Front Pharmacol. 2023 May 23;14:1196158. doi: 10.3389/fphar.2023.1196158. eCollection 2023.
5
Thiazole, Isatin and Phthalimide Derivatives Tested against Cancer Models: A Literature Review of the Last Six Years.噻唑、靛红和邻苯二甲酰亚胺衍生物的抗癌模型测试：对过去六年文献的综述。
Curr Med Chem. 2024;31(20):2991-3032. doi: 10.2174/0929867330666230426154055.
6
New benzothiazole hybrids as potential VEGFR-2 inhibitors: design, synthesis, anticancer evaluation, and study.新型苯并噻唑类杂合体作为潜在的 VEGFR-2 抑制剂：设计、合成、抗癌评价及研究。
J Enzyme Inhib Med Chem. 2023 Dec;38(1):2166036. doi: 10.1080/14756366.2023.2166036.
7
Synthesis and Antimicrobial, Anticancer and Anti-Oxidant Activities of Novel 2,3-Dihydropyrido[2,3-d]pyrimidine-4-one and Pyrrolo[2,1-b][1,3]benzothiazole Derivatives via Microwave-Assisted Synthesis.新型 2,3-二氢吡啶并[2,3-d]嘧啶-4(1H)-酮和吡咯并[2,1-b][1,3]苯并噻唑衍生物的微波辅助合成及抗菌、抗癌和抗氧化活性。
Molecules. 2022 Feb 12;27(4):1246. doi: 10.3390/molecules27041246.
8
Importance of Fluorine in Benzazole Compounds.苯并唑类化合物中氟的重要性。
Molecules. 2020 Oct 14;25(20):4677. doi: 10.3390/molecules25204677.
9
Benzothiazole derivatives as anticancer agents.苯并噻唑衍生物作为抗癌剂。
J Enzyme Inhib Med Chem. 2020 Dec;35(1):265-279. doi: 10.1080/14756366.2019.1698036.
10
A Fluorinated Phenylbenzothiazole Arrests the Trypanosoma cruzi Cell Cycle and Diminishes the Infection of Mammalian Host Cells.一种氟化苯并噻唑抑制克氏锥虫细胞周期并减少对哺乳动物宿主细胞的感染。
Antimicrob Agents Chemother. 2020 Jan 27;64(2). doi: 10.1128/AAC.01742-19.