• 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

基于结构的吡唑并[1,5-a][1,3,5]三嗪衍生物的设计、合成及其作为蛋白激酶CK2强效抑制剂的研究

Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2.

作者信息

Nie Zhe, Perretta Carin, Erickson Philip, Margosiak Stephen, Almassy Robert, Lu Jia, Averill April, Yager Kraig M, Chu Shaosong

机构信息

Department of Medicinal Chemistry, Polaris Pharmaceuticals Inc., San Diego, CA 92121, USA.

出版信息

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4191-5. doi: 10.1016/j.bmcl.2007.05.041. Epub 2007 May 18.

DOI:10.1016/j.bmcl.2007.05.041
PMID:17540560
Abstract

The structure-based design, synthesis, and anticancer activity of novel inhibitors of protein kinase CK2 are described. Using pyrazolo[1,5-a][1,3,5]triazine as the core scaffold, a structure-guided series of modifications provided pM inhibitors with microM-level cytotoxic activity in cell-based assays with prostate and colon cancer cell lines.

摘要

描述了基于结构的蛋白激酶CK2新型抑制剂的设计、合成及抗癌活性。以吡唑并[1,5-a][1,3,5]三嗪为核心骨架，通过一系列基于结构的修饰，得到了在前列腺和结肠癌细胞系的细胞实验中具有微摩尔级细胞毒性活性的皮摩尔级抑制剂。

相似文献

1
Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2.基于结构的吡唑并[1,5-a][1,3,5]三嗪衍生物的设计、合成及其作为蛋白激酶CK2强效抑制剂的研究
Bioorg Med Chem Lett. 2007 Aug 1;17(15):4191-5. doi: 10.1016/j.bmcl.2007.05.041. Epub 2007 May 18.
2
Structure-based design and synthesis of novel macrocyclic pyrazolo[1,5-a] [1,3,5]triazine compounds as potent inhibitors of protein kinase CK2 and their anticancer activities.基于结构的新型大环吡唑并[1,5-a][1,3,5]三嗪化合物的设计与合成及其作为蛋白激酶CK2强效抑制剂的抗癌活性
Bioorg Med Chem Lett. 2008 Jan 15;18(2):619-23. doi: 10.1016/j.bmcl.2007.11.074. Epub 2007 Nov 28.
3
Identification of polyoxometalates as nanomolar noncompetitive inhibitors of protein kinase CK2.多金属氧酸盐作为蛋白激酶CK2的纳摩尔级非竞争性抑制剂的鉴定。
Chem Biol. 2008 Jul 21;15(7):683-92. doi: 10.1016/j.chembiol.2008.05.018.
4
Urolithin as a converging scaffold linking ellagic acid and coumarin analogues: design of potent protein kinase CK2 inhibitors.尿石素作为连接鞣花酸和香豆素类似物的汇聚支架：强效蛋白激酶 CK2 抑制剂的设计。
ChemMedChem. 2011 Dec 9;6(12):2273-86. doi: 10.1002/cmdc.201100338. Epub 2011 Oct 4.
5
New protein kinase CK2 inhibitors: jumping out of the catalytic box.新型蛋白激酶CK2抑制剂：跳出催化框
Chem Biol. 2009 Feb 27;16(2):112-20. doi: 10.1016/j.chembiol.2009.01.004.
6
Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors.用于新型激酶抑制剂开发的通用模板：新型CDK抑制剂的发现
Bioorg Med Chem Lett. 2007 Nov 15;17(22):6216-9. doi: 10.1016/j.bmcl.2007.09.018. Epub 2007 Sep 8.
7
Synthesis and biological evaluation of substituted (thieno[2,3-d]pyrimidin-4-ylthio)carboxylic acids as inhibitors of human protein kinase CK2.取代（噻吩并[2,3-d]嘧啶-4-基硫代）羧酸的合成及作为人蛋白激酶 CK2 抑制剂的生物评价。
Eur J Med Chem. 2011 Mar;46(3):870-6. doi: 10.1016/j.ejmech.2010.12.025. Epub 2011 Jan 9.
8
Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors.作为Raf激酶抑制剂的口服生物可利用苯并咪唑的设计与合成。
J Med Chem. 2008 Nov 27;51(22):7049-52. doi: 10.1021/jm801050k.
9
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.吡唑并嘧啶类：一种用于高效选择性p38α抑制剂的新型杂环骨架。
Bioorg Med Chem Lett. 2008 Apr 15;18(8):2652-7. doi: 10.1016/j.bmcl.2008.03.019. Epub 2008 Mar 10.
10
Diversity-oriented synthesis of pyrazolo[4,3-b]indoles by gold-catalysed three-component annulation: application to the development of a new class of CK2 inhibitors.通过金催化的三组分环化反应进行吡唑并[4,3-b]吲哚的多样性导向合成：在新型 CK2 抑制剂开发中的应用。
Org Biomol Chem. 2013 May 28;11(20):3288-96. doi: 10.1039/c3ob40223a.

引用本文的文献

1
Synthesis, anticancer evaluation, and electrochemical investigation of new chiral pyrazolo[4,3-e]tetrazolo[1,5-b][1,2,4]triazine sulfonamides.新型手性吡唑并[4,3-e]四唑并[1,5-b][1,2,4]三嗪磺酰胺的合成、抗癌活性评价及电化学研究
Sci Rep. 2025 May 28;15(1):18640. doi: 10.1038/s41598-025-02835-w.
2
Recent Developments and Future Perspectives of Purine Derivatives as a Promising Scaffold in Drug Discovery.嘌呤衍生物作为药物发现中一种有前景的骨架的最新进展与未来展望
Curr Top Med Chem. 2024;24(6):541-579. doi: 10.2174/0115680266290152240110074034.
3
6-(Tetrazol-5-yl)-7-aminoazolo[1,5-]pyrimidines as Novel Potent CK2 Inhibitors.
6-(四唑-5-基)-7-氨基氮杂[1,5-a]嘧啶类化合物作为新型有效的 CK2 抑制剂。
Molecules. 2022 Dec 8;27(24):8697. doi: 10.3390/molecules27248697.
4
Host Kinase CSNK2 is a Target for Inhibition of Pathogenic SARS-like β-Coronaviruses.宿主激酶 CSNK2 是抑制致病 SARS 样 β-冠状病毒的靶标。
ACS Chem Biol. 2022 Jul 15;17(7):1937-1950. doi: 10.1021/acschembio.2c00378. Epub 2022 Jun 19.
5
Preparation of Novel Pyrazolo[4,3-]tetrazolo[1,5-][1,2,4]triazine Sulfonamides and Their Experimental and Computational Biological Studies.新型吡唑并[4,3-]四唑并[1,5-][1,2,4]三嗪磺酰胺的制备及其实验和计算生物学研究。
Int J Mol Sci. 2022 May 24;23(11):5892. doi: 10.3390/ijms23115892.
6
Synthesis of new pyrazolo[1,2,3]triazines by cyclative cleavage of pyrazolyltriazenes.通过吡唑基三氮烯的环化裂解合成新型吡唑并[1,2,3]三嗪
Beilstein J Org Chem. 2021 Nov 22;17:2773-2780. doi: 10.3762/bjoc.17.187. eCollection 2021.
7
Microwave-Assisted Sequential One-Pot Synthesis of 8-Substituted Pyrazolo[1,5-][1,3,5]triazines.微波辅助顺序一锅法合成 8-取代吡唑并[1,5-][1,3,5]三嗪。
Molecules. 2021 Jun 10;26(12):3540. doi: 10.3390/molecules26123540.
8
Protein kinase CK2: a potential therapeutic target for diverse human diseases.蛋白激酶 CK2：一种针对多种人类疾病的潜在治疗靶点。
Signal Transduct Target Ther. 2021 May 17;6(1):183. doi: 10.1038/s41392-021-00567-7.
9
Downfalls of Chemical Probes Acting at the Kinase ATP-Site: CK2 as a Case Study.作用于激酶 ATP 结合位点的化学探针的局限性：以 CK2 为例。
Molecules. 2021 Mar 31;26(7):1977. doi: 10.3390/molecules26071977.
10
Computational Macrocyclization: From de novo Macrocycle Generation to Binding Affinity Estimation.计算大环化：从从头大环生成到结合亲和力估计
ChemMedChem. 2017 Nov 22;12(22):1866-1872. doi: 10.1002/cmdc.201700478. Epub 2017 Oct 25.