CAS: 15862-34-7; 5-Bromo-2-Hydroxy-3-Nitropyridine

相似化合物

186413-74-1 6332-56-5 153888-45-0

上下游产品

5-bromo-2-pyridylamine 2-hydroxy-3-nitropyridine 5-bromo-3-nitro-pyridin-2-ylamine sulfuric acid 5-bromo-2-hydroxy-3-aminopyridine 5-bromo-2-chloro-3-nitropyridine 2,5-dibromo-3-nitro-pyridine 5-bromo-2-methoxy-3-nitropyridine

2-氨基-5-溴-3-硝基吡啶置于硫酸,Sodium Nitrite体系中,用 水 用作溶剂,以82%的收率获得5-溴-2-羟基-3-硝基吡啶
参考文献:含烷基磺酰胺的喹唑啉衍生物作为有效的和口服可生物利用的pi3Ks抑制剂.
标题:含烷基磺酰胺的喹唑啉衍生物作为有效的和口服可生物利用的pi3Ks抑制剂.
摘要:磷酸肌醇3-激酶(pi3Ks)被认为是治疗各种癌症的有希望的靶标,因为它们在调节细胞增殖,分化,迁移和存活中的作用.在这里,我们报告了我们为开发有效的和口服可生物利用的pi3K抑制剂来治疗癌症的努力.含烷基磺酰胺的喹唑啉衍生物a1-A18显着抑制pi3Kα,并抑制hct-116,Mcf-7和su-Dhl-6细胞系之间的细胞增殖.最佳化合物a1对pi3Kα(ic 50 = 4.5 Nm),Pi3Kβ(ic 50 = 4.5 Nm),Pi3Kγ(ic 50 = 4.5 Nm),Pi3Kδ(ic 50 = 4.5 Nm),并显着抑制hct-116,Mcf-7和su-Dhl-6细胞系的生长,Ic 50值分别为0.82 µm,0.99 µm和0.19 µm.蛋白质印迹分析表明,A1以剂量依赖性方式显着抑制akt S473的磷酸化.此外,在裸鼠hct-116异种移植模型中,A1在体内剂量为25 Mg
Doi:10.1016/j.Bmc.2019.05.043

专利信息

专利号:US-8404670-B2
优先权日:2009-02-11
标题:Histamine H3 inverse agonists and antagonists and methods of use thereof
发明人：CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SPEAR KERRY L
权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SPEAR KERRY L; SUNOVION PHARMACEUTICALS INC
摘要:Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

专利号:CN-108570001-A
优先权日:2017-03-08
标 题:A kind of synthesis and its application of 3- amino -2 hydroxy pyrimidine