CAS: 1423-61-6; 7-Bromobenzo[b]Thiophene

相似化合物

4923-87-9 17347-32-9 7342-82-7

上下游产品

7-溴-1-苯并噻吩-2-羧酸 7-Bromobenzo[b]Thiophene-2-Carboxylic Acid 19075-59-3

7-溴-1-苯并噻吩-2-羧酸置于溶剂黄146,Silver Carbonate体系中,用 二甲基亚砜 用作溶剂,化学反应 16.0H,以76%的收率获得7-溴苯并[b]噻吩
参考文献:Antagonizing Stat3 Activation With Benzo[b]Thiophene 1,1-Dioxide Based Small Molecules
标题:Antagonizing Stat3 Activation With Benzo[b]Thiophene 1,1-Dioxide Based Small Molecules
摘要:Stat3 Is An Attractive Therapeutic Target For Cancer Therapy. However,Due To Low Potency Or Poor Druggability,None Of Its Inhibitors Are Clinically Available. Herein,A Series Of Aminobenzo[b]Thiophene 1,1-Dioxides With Good Drug-Likeness Properties Were Designed,Synthesized And Evaluated As Stat3 Inhibitors. Most Of Them Exhibited Higher Antitumor Activity Than The Small-Molecule Stat3 Inhibitor,Stattic. Compound 15 Was The Most Potent And Had An Ic50 Range In 0.33-0.75 Mu M In Various Cancer Cell Lines. The Overexpressed And Il-6 Induced Phosphorylation Levels Of Stat3 Were Both Inhibited By 15 Without Influencing The Phosphorylation Levels Of The Upstream Kinases Src And Jak2. 15 Also Suppressed The Expressions Of Stat3 Downstream Gene,Bcl-2. 15 Effectively Increased The Ros Levels Of Cancer Cells,Induced Cancer Cell Apoptosis And Abolished The Colony Formation Ability Of Cancer Cells Without Affecting Bypass Kinase P-Erk. Furthermore,15 In Vivo Induced Significant Antitumor Responses,And Exhibited Less Toxicity Than Doxorubicin. Together,This Study Described A Class Of New Stat3 Inhibitors As Antitumor Agents. (C) 2016 Elsevier Masson Sas. All Rights Reserved.
Doi:10.1016/j.Ejmech.2016.09.068

专利信息

专利号:CN-114605378-B
优先权日:2022-03-24
标 题 :A kind of thiophene fused ring compound and its synthesis method and application