• 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

新型 D 环稠合甾体杂环的设计与合成。

Design and synthesis of novel D-ring fused steroidal heterocycles.

机构信息

School of Pharmaceutical Sciences and New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, PR China.

出版信息

Steroids. 2013 Dec 11;78(12-13):1200-8. doi: 10.1016/j.steroids.2013.07.006. Epub 2013 Aug 1.

DOI:10.1016/j.steroids.2013.07.006
PMID:23911850
Abstract

Using dehydroepiandrosterone as the starting material, we have synthesized a series of steroid analogs possessing a D-ring fused with heterocycles which are pyridine, imidazo [2,1-b]thiazoles or substituted thiazole imines. All the final structures are first reported and identified by NMR and MS spectroscopys, the yields of these products are moderate to good and the reaction conditions are mild. The cytotoxicity of the synthesized compounds against EC-109(human esophageal carcinoma), EC-9706(human esophageal carcinoma), MGC-803(human gastric carcinoma) were investigated.

摘要

以脱氢表雄酮为起始原料，我们合成了一系列具有 D 环与杂环稠合的甾体类似物，其中杂环为吡啶、咪唑并[2,1-b]噻唑或取代噻唑亚胺。所有最终结构均经 NMR 和 MS 光谱首次确证，这些产物的产率为中等到良好，反应条件温和。合成化合物对 EC-109（人食管癌细胞）、EC-9706（人食管癌细胞）、MGC-803（人胃癌细胞）的细胞毒性进行了研究。

相似文献

1
Design and synthesis of novel D-ring fused steroidal heterocycles.新型 D 环稠合甾体杂环的设计与合成。
Steroids. 2013 Dec 11;78(12-13):1200-8. doi: 10.1016/j.steroids.2013.07.006. Epub 2013 Aug 1.
2
Synthesis and biological evaluation of dehydroepiandrosterone-fused thiazole, imidazo[2,1-b]thiazole, pyridine steroidal analogues.脱氢表雄酮稠合噻唑、咪唑并[2,1 - b]噻唑、吡啶甾体类似物的合成及生物学评价
Steroids. 2014 Feb;80:92-101. doi: 10.1016/j.steroids.2013.12.003. Epub 2013 Dec 16.
3
Synthesis, characterization, and cytotoxicity of some novel glycosyl thiazol-2-imines as antitumoral agents.一些新型糖基噻唑-2-亚胺的合成、表征及其作为抗肿瘤剂的细胞毒性。
Carbohydr Res. 2010 Feb 11;345(3):437-41. doi: 10.1016/j.carres.2009.11.032. Epub 2009 Dec 5.
4
Synthesis, antiproliferative and antiviral activity of imidazo[4,5-d]isothiazole nucleosides as 5:5 fused analogs of nebularine and 6-methylpurine ribonucleoside.咪唑并[4,5-d]异噻唑核苷作为杀稻瘟菌素和6-甲基嘌呤核糖核苷的5:5稠合类似物的合成、抗增殖及抗病毒活性
J Med Chem. 1997 Feb 28;40(5):771-84. doi: 10.1021/jm960605z.
5
Synthesis and anticancer activity of novel 3,4-diarylthiazol-2(3H)-ones (imines).新型3,4-二芳基噻唑-2(3H)-酮（亚胺）的合成及其抗癌活性
Bioorg Med Chem Lett. 2009 Oct 1;19(19):5661-4. doi: 10.1016/j.bmcl.2009.08.025. Epub 2009 Aug 8.
6
FeCl3/ZnI2-catalyzed synthesis of benzo[d]imidazo[2,1-b]thiazole through aerobic oxidative cyclization between 2-aminobenzothiazole and ketone.FeCl₃/ZnI₂催化2-氨基苯并噻唑与酮通过有氧氧化环化反应合成苯并[d]咪唑并[2,1-b]噻唑。
Org Lett. 2014 Dec 5;16(23):6084-7. doi: 10.1021/ol5028893. Epub 2014 Nov 13.
7
Transition-metal-free synthesis of imidazo[2,1-b]thiazoles and thiazolo[3,2-a]benzimidazoles via an S-propargylation/5-exo-dig cyclization/isomerization sequence using propargyl tosylates as substrates.以炔丙基甲苯磺酸酯为底物，通过S-炔丙基化/5-外向-环化/异构化序列无过渡金属合成咪唑并[2,1-b]噻唑和噻唑并[3,2-a]苯并咪唑。
J Org Chem. 2014 Nov 7;79(21):10367-77. doi: 10.1021/jo501980w. Epub 2014 Oct 16.
8
Design, synthesis, and biological activity of thiazole derivatives as novel influenza neuraminidase inhibitors.设计、合成及噻唑衍生物作为新型流感神经氨酸酶抑制剂的生物活性。
J Enzyme Inhib Med Chem. 2011 Aug;26(4):506-13. doi: 10.3109/14756366.2010.534732. Epub 2010 Dec 14.
9
Asymmetric Mannich reactions of imidazo[2,1-b]thiazole-derived nucleophiles with (S(S))-N-tert-butanesulfinyl (3,3,3)-trifluoroacetaldimine.咪唑并[2,1-b]噻唑衍生亲核试剂与(S(S))-叔丁基亚磺酰基(3,3,3)-三氟乙二亚胺的不对称 Mannich 反应。
Org Biomol Chem. 2013 Dec 14;11(46):8018-21. doi: 10.1039/c3ob41785a.
10
Heterocycles 27. Microwave assisted synthesis and antitumour activity of novel phenothiazinyl-thiazolyl-hydrazine derivatives.杂环化合物 27. 新型吩噻嗪基-噻唑基-腙衍生物的微波辅助合成及抗肿瘤活性。
Arch Pharm (Weinheim). 2012 Jul;345(7):574-83. doi: 10.1002/ardp.201100355. Epub 2012 Apr 25.

引用本文的文献

1
Synthesis, biological activities, and future perspectives of steroidal monocyclic pyridines.甾体单环吡啶的合成、生物活性及未来展望
RSC Med Chem. 2023 Sep 7;14(10):1934-1972. doi: 10.1039/d3md00411b. eCollection 2023 Oct 18.
2
Multistep Synthesis and In Vitro Anticancer Evaluation of 2-Pyrazolyl-Estradiol Derivatives, Pyrazolocoumarin-Estradiol Hybrids and Analogous Compounds.2-吡唑基雌二醇衍生物、吡唑并香豆素-雌二醇杂合体及类似物的多步合成及体外抗癌活性评价。
Molecules. 2020 Sep 4;25(18):4039. doi: 10.3390/molecules25184039.
3
Synthesis, Characterization, and Evaluation of Cytotoxic Effects of Novel Hybrid Steroidal Heterocycles as PEG Based Nanoparticles.
新型杂化甾体杂环作为基于聚乙二醇的纳米颗粒的合成、表征及细胞毒性作用评估
Asian Pac J Cancer Prev. 2017 Jul 27;18(7):1937-1946. doi: 10.22034/APJCP.2017.18.7.1937.
4
Structurally novel steroidal spirooxindole by241 potently inhibits tumor growth mainly through ROS-mediated mechanisms.新型甾体螺环氧化吲哚化合物 241 通过 ROS 介导的机制强烈抑制肿瘤生长。
Sci Rep. 2016 Aug 16;6:31607. doi: 10.1038/srep31607.
5
Synthesis and in vitro antiproliferative evaluation of some B-norcholesteryl Benzimidazole and Benzothiazole derivatives.某些B-去甲胆固醇基苯并咪唑和苯并噻唑衍生物的合成及体外抗增殖活性评价
Mar Drugs. 2015 Apr 22;13(4):2488-504. doi: 10.3390/md13042488.