📜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