CAS: 1226056-71-8; N-Benzyl-2-(Pyrimidin-4-Ylamino)Thiazole-4-Carboxamide

该化合物是一种小分子化合物,其作用是选择性抑制蛋白质直流酶GSK-3(甘烃合成酶3),主要被确认为在干细胞研究中的潜在应用,特别是在提高将体细胞重新编程到诱导多功能干细胞(iPSCs)的效率方面.Thiazovivin功能通过调制影响细胞命运和多功能的信号路径来调节Thiazovivin功能.该化合物的特征是其促进其生物活动的硫酸环结构.该化合物通常在实验室环境中施用,其效果在各种细胞环境中研究.许多化学物质,安全和处理防范措施都必不可少,因为硫焦维因浓度和接触而可能有具体的毒性特征.

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CAS号163133-86-6 4(1H)-Pyrimidin...

合成工艺路线路线简述

    📜在 三氟乙酸体系中,用 二氯甲烷 用作溶剂,化学反应 6.0H,以52.1%的收率获得n-苄基-2-(嘧啶-4-基氨基)噻唑-4-羧酰胺
    参考文献:一种离子液体及利用其合成thiazovivin的方 法
    标题:一种离子液体及利用其合成thiazovivin的方 法
    摘要:本发明提供一种用于合成thiazovivin的离子液体,属于有机合成技术领域.所述离子液体具有如下通式1所示的结构:本发明还提供一种基于上述离子液体的thiazovivin合成方法,包括(1)将所述离子液体与苄胺连接得到化合物4;(2)将上述化合物4与2‑溴噻唑‑4‑羧酸进行酰化反应得到化合物5;(3)上述化合物5与4‑氨基嘧啶进行胺化反应得到化合物6;(4)将上述化合物6中的离子液体去掉即可得到所述thiazovivin.

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    专利信息


    专利号:US-2017283878-A1
    优先权日:2015-12-11
    标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
    发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
    权利人:ACADEMIA SINICA
    摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

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    主要参考文献


    1: Sharifi-Kelishadi M, Zare L, Fathollahi Y, Javan M. Conversion of Astrocyte Cell Lines to Oligodendrocyte Progenitor Cells Using Small Molecules and Transplantation to Animal Model of Multiple Sclerosis. J Mol Neurosci. 2024 Apr 9;74(2):40. doi: 10.1007/s12031-024-02206-6.
    174:116435. doi: 10.1016/j.biopha.2024.116435. Epub 2024 Mar 20. 12(1):17811. doi: 10.1038/s41598-022-21610-9.
    4: Samoilova EM, Revkova VA, Brovkina OI, Kalsin VA, Melnikov PA, Konoplyannikov MA, Galimov KR, Nikitin AG, Troitskiy AV, Baklaushev VP. Chemical Reprogramming of Somatic Cells in Neural Direction: Myth or Reality? Bull Exp Biol Med. 2019 Aug;167(4):546-555. doi: 10.1007/s10517-019-04570-5. Epub 2019 Sep 9. 1(6):2054-2061. doi: 10.1021/acsabm.8b00528. Epub 2018 Nov 13.

    合成参考文献


    参考文献:10.1124/mol.119.115964
    摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
    参考文献:10.3892/ijmm.2017.3103
    摘要:Wu Q, Ouyang C, Xie L, Ling Y, Huang T. The ROCK inhibitor, thiazovivin, inhibits human corneal endothelial‑to‑mesenchymal transition/epithelial‑to‑mesenchymal transition and increases ionic transporter expression. Int J Mol Med. 2017 Oct;40(4):1009–18.
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