CAS: 1123738-15-7; 3-Bromoquinolin-5-Ol

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145369-94-4 57798-00-2 1160949-99-4

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CAS号116632-33-8 3-溴-5-硝基喹啉 | CAS号116632-57-6 3-溴-5-氨基喹啉 | CAS号607-34-1 5-硝基喹啉

📜3-溴-5-硝基喹啉置于铁粉,溶剂黄146,硫酸,Sodium Nitrite,水体系中,用 水 用作溶剂,以30%的收率获得3-溴-5-羟基喹啉
参考文献:Synthesis And C-Met Kinase Inhibition Of 3,5-Disubstituted And 3,5,7-Trisubstituted Quinolines: Identification Of 3-(4-Acetylpiperazin-1-yl)-5-(3-Nitrobenzylamino)-7-(Trifluoromethyl)Quinoline As A Novel Anticancer Agent
标题:Synthesis And C-Met Kinase Inhibition Of 3,5-Disubstituted And 3,5,7-Trisubstituted Quinolines: Identification Of 3-(4-Acetylpiperazin-1-yl)-5-(3-Nitrobenzylamino)-7-(Trifluoromethyl)Quinoline As A Novel Anticancer Agent
摘要:By Use Of An Improved Synthetic Strategy,A Series Of 3,5-Disubstituted And 3,5,7-Trisubstituted Quinolines Were Readily Prepared. 3,5,7-Trisubstituted Quinolines 21A-C,211,And 27A-C Were Identified As The Most Potent C-Met Inhibitors With Ic50 Of Less Than 1.0 Nm. Compound 21B Showed The Most Promising Overall Pk Profile And Has High Potency And Extraordinary Selectivity To C-Met Against C-Met Family Member Ron And 12 Other Tyrosine Kinases. It Produced Constitutive Inhibition Of C-Met Phosphorylation In C-Met Dependent Cell Lines. At Doses Of 100 Mg/kg,Compound 21B Showed Statistically Significant Tumor Growth Inhibition (68-69%) In Both Nih-3T3-Tpr-Met And U-87 Mg Human Gliobastoma Xenograft Models. These Results Clearly Indicated That Compound 21B Is A Potent And Highly Selective C-Met Inhibitor. Its Favorable In Vitro And In Vivo Profiles Warrant Further Investigation.
Doi:10.1021/jm101340Q