• 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

3,4-二取代-5-(3,4,5-三甲氧基苯基)-4H-1,2,4-三唑和新型含 3,4,5-三甲氧基苯基部分的 5,6-二氢-[1,2,4]三唑并[3,4-b][1,3,4]噻二唑衍生物的合成及细胞毒性。

Synthesis and cytotoxicity of 3,4-disubstituted-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazoles and novel 5,6-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives bearing 3,4,5-trimethoxyphenyl moiety.

机构信息

Department of Chemistry, College of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, PR China.

出版信息

Bioorg Med Chem Lett. 2012 Jul 1;22(13):4471-4. doi: 10.1016/j.bmcl.2012.03.023. Epub 2012 Mar 11.

DOI:10.1016/j.bmcl.2012.03.023
PMID:22647723
Abstract

A series of 3,4-disubstituted-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazoles and some novel 5,6-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles bearing 3,4,5-trimethoxyphenyl moiety were synthesized and screened for their anticancer activity. The preliminary bioassay results indicated that compounds 14 and 16 showed much stronger cytotoxicity than Doxorubicin against HepG2 cell lines with IC(50) values of 0.58 and 3.17 μM, respectively. Meanwhile compound 16 also exhibited a broad spectrum of antitumor activity against MCF-7 and MKN45 with IC(50) values of 10.92 and 13.79 μM, respectively.

摘要

一系列 3,4-二取代-5-(3,4,5-三甲氧基苯基)-4H-1,2,4-三唑和一些新型含 3,4,5-三甲氧基苯基部分的 5,6-二氢-[1,2,4]三唑并[3,4-b][1,3,4]噻二唑被合成并筛选其抗癌活性。初步的生物测定结果表明，化合物 14 和 16 对 HepG2 细胞系的细胞毒性比阿霉素强得多，IC50 值分别为 0.58 和 3.17 μM。同时，化合物 16 对 MCF-7 和 MKN45 也表现出广谱的抗肿瘤活性，IC50 值分别为 10.92 和 13.79 μM。

相似文献

1
Synthesis and cytotoxicity of 3,4-disubstituted-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazoles and novel 5,6-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives bearing 3,4,5-trimethoxyphenyl moiety.3,4-二取代-5-(3,4,5-三甲氧基苯基)-4H-1,2,4-三唑和新型含 3,4,5-三甲氧基苯基部分的 5,6-二氢-[1,2,4]三唑并[3,4-b][1,3,4]噻二唑衍生物的合成及细胞毒性。
Bioorg Med Chem Lett. 2012 Jul 1;22(13):4471-4. doi: 10.1016/j.bmcl.2012.03.023. Epub 2012 Mar 11.
2
Synthesis and antiproliferative activity of some new thieno[2,3-d]pyrimidin-4(3H)-ones containing 1,2,4-triazole and 1,3,4-thiadiazole moiety.一些含有1,2,4-三唑和1,3,4-噻二唑部分的新型噻吩并[2,3-d]嘧啶-4(3H)-酮的合成及抗增殖活性
Eur J Med Chem. 2014 Oct 30;86:676-83. doi: 10.1016/j.ejmech.2014.09.032. Epub 2014 Sep 10.
3
Synthesis and biological evaluation of 1,2,4-triazole and 1,3,4-thiadiazole derivatives as potential cytotoxic agents.
Chem Pharm Bull (Tokyo). 2013;61(11):1099-104. doi: 10.1248/cpb.c13-00242. Epub 2013 Aug 10.
4
Benzimidazole clubbed with triazolo-thiadiazoles and triazolo-thiadiazines: new anticancer agents.苯并咪唑与三唑并噻二唑和三唑并噻嗪结合：新型抗癌剂。
Eur J Med Chem. 2013 Apr;62:785-98. doi: 10.1016/j.ejmech.2012.07.011. Epub 2012 Jul 16.
5
Synthesis of novel indolyl-1,2,4-triazoles as potent and selective anticancer agents.合成新型吲哚基-1,2,4-三唑类化合物作为有效的选择性抗癌药物。
Chem Biol Drug Des. 2011 Mar;77(3):182-8. doi: 10.1111/j.1747-0285.2010.01051.x. Epub 2011 Jan 19.
6
Benzimidazole bearing oxadiazole and triazolo-thiadiazoles nucleus: design and synthesis as anticancer agents.苯并咪唑类含恶二唑和三唑并噻二唑核：作为抗癌剂的设计与合成。
Bioorg Med Chem Lett. 2012 Sep 1;22(17):5438-44. doi: 10.1016/j.bmcl.2012.07.038. Epub 2012 Jul 17.
7
Synthesis and anticonvulsant activities of some triazolothiadiazole derivatives.一些三唑并噻二唑衍生物的合成及抗惊厥活性。
Arch Pharm (Weinheim). 2012 Jul;345(7):565-73. doi: 10.1002/ardp.201100326. Epub 2012 Apr 25.
8
Synthesis of novel 1,2,4-triazoles, triazolothiadiazines and triazolothiadiazoles as potential anticancer agents.新型1,2,4-三唑、三唑并噻二嗪和三唑并噻二唑作为潜在抗癌剂的合成。
Eur J Med Chem. 2014 Oct 30;86:75-80. doi: 10.1016/j.ejmech.2014.08.047. Epub 2014 Aug 15.
9
In-vitro anti-HIV and antitumor activity of new 3,6-disubstituted [1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles and thiadiazine analogues.新型3,6-二取代[1,2,4]三唑并[3,4-b][1,3,4]噻二唑及噻二嗪类似物的体外抗HIV和抗肿瘤活性
Arch Pharm (Weinheim). 2008 Jun;341(6):365-9. doi: 10.1002/ardp.200700272.
10
Synthesis of some new [1,2,4]triazolo[3,4-b][1,3,4]thiadiazines and [1,2,4]triazolo[3,4-b][1,3,4] thiadiazoles starting from 5-nitro-2-furoic acid and evaluation of their antimicrobial activity.从 5-硝基-2-糠酸出发合成一些新的[1,2,4]三唑并[3,4-b][1,3,4]噻二嗪和[1,2,4]三唑并[3,4-b][1,3,4]噻二唑，并评价它们的抗菌活性。
Bioorg Med Chem. 2011 Aug 1;19(15):4506-12. doi: 10.1016/j.bmc.2011.06.024. Epub 2011 Jun 16.

引用本文的文献

1
An insight on medicinal attributes of 1,2,4-triazoles.对 1,2,4-三唑药用属性的深入了解。
Eur J Med Chem. 2020 Nov 1;205:112652. doi: 10.1016/j.ejmech.2020.112652. Epub 2020 Jul 27.
2
Cell-based screen identifies a new potent and highly selective CK2 inhibitor for modulation of circadian rhythms and cancer cell growth.基于细胞的筛选鉴定出一种新型有效的、高选择性的 CK2 抑制剂，可用于调节昼夜节律和癌细胞生长。
Sci Adv. 2019 Jan 23;5(1):eaau9060. doi: 10.1126/sciadv.aau9060. eCollection 2019 Jan.