CAS: 1001753-24-7; N-(4-Mesitylthiazol-2-yl)Benzamide

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4-(2,4,6-trimethylphenyl)thiazol-2-ylamine benzoyl chlorideN-(2-{2-[2-(2-azido-ethoxy)-ethoxy]-ethoxy}-ethyl)-N-[4-(2,4,6-trimethyl-phenyl)-thiazol-2-yl]benzamide {benzoyl-[4-(2,4,6-trimethylphenyl)thiazol-2-yl]-amino}acetic acid ethyl ester N-methyl-N-[4-(2,4,6-trimethylphenyl)thiazol-2-yl]benzamide

合成工艺路线路线简述

    📜4-(2,4,6-三甲基苯基)-2-氨基噻唑,苯甲酰氯置于三乙胺体系中,用 1,4-二氧六环 用作溶剂,化学反应 2.5H,以31%的收率获得n-[4-(2,4,6-三甲基苯基)-2-噻唑基]苯甲酰胺
    参考文献:Synthesis And Biological Evaluation Of A Series Of Novel Inhibitor Of Nek2/hec1 Analogues
    标题:Synthesis And Biological Evaluation Of A Series Of Novel Inhibitor Of Nek2/hec1 Analogues
    摘要:High Expression In Cancer 1 (Hec1) Is An Oncogene Overly Expressed In Many Human Cancers. Small Molecule Inhibitor Of Nek2/hcc1 (Inh) Targeting The Heel And Its Regulator,Nek2,In The Mitotic Pathway,Was Identified To Inactivate Hec1/nek2 Function Mediated By Protein Degradation That Subsequently Leads To Chromosome Mis-Segregation And Cell Death. To Further Improve The Efficacy Of Inh,A Series Of Inh Analogues Were Designed,Synthesized,And Evaluated. Among These 33 Newly Synthesized Analogues,Three Of Them,6,13,And 21,Have 6-8 Fold More Potent Cell Killing Activity Than The Previous Lead Compound Inh1. Compounds 6 And 21 Were Chosen For Analyzing The Underlying Action Mechanism. They Target Directly The Hec1/nek2 Pathway And Cause Chromosome Mis-Alignment As Well As Cell Death,A Mechanism Similar To That Of Inh1,This Initial Exploration Of Structural/functional Relationship Of Inh May Advance The Progress For Developing Clinically Applicable Inh Analogue.
    Doi:10.1021/jm8015969

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    主要参考文献


    1: Pease C, Hutton B, Yazdi F, Wolfe D, Hamel C, Quach P, Skidmore B, Moher D, Alvarez GG. Efficacy and completion rates of rifapentine and isoniazid (3HP) compared to other treatment regimens for latent tuberculosis infection: a systematic review with network meta-analyses. BMC Infect Dis. 2017 Apr 11;17(1):265. doi: 10.1186/s12879-017-2377-x. Review.
    2: Niu Y, Song Y, Hou H, Zhu Y. Synthesis, structure, and large optical limiting effect of the first coordination polymeric cluster based on an {I@[AgI(inh)]6} hexagram block. Inorg Chem. 2005 Apr 4;44(7):2553-9.

    合成参考文献

    合成方法参考DOI号:10.1021/jm8015969
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