CAS: 405224-22-8; 5-Bromo-2-Oxo-1,2-Dihydropyridine-3-Carbonitrile

相似化合物

914482-23-8 1951442-01-5 914224-28-5

上下游产品

pyrid-2-one-3-carbonitrile 2-chloro-3-pyridinecarbonitrile 2-hydroxy-3-cyanopyridine 5-bromo-2-chloropyridine-3-carbonitrile 5-bromo-1H-pyrazolo[3,4-b]pyridine-3-amine N-(5-bromo-1H-pyrazolo[3,4-b]pyridin-3-yl)butyramide N-[5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-butyramideN-[5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-butyramide

2-氯-3-氰基吡啶置于溴,溶剂黄146体系中,化学反应 11.5H,反应生成 5-溴-3-氰基-2(1H)-吡啶酮
参考文献:基于片段的n-取代-5-(4-异丙基硫代苯酚)-2-羟基烟酰胺衍生物作为新型mcl-1抑制剂的设计,合成和生物学评估
标题:基于片段的n-取代-5-(4-异丙基硫代苯酚)-2-羟基烟酰胺衍生物作为新型mcl-1抑制剂的设计,合成和生物学评估
摘要:我们先前已经报道了抗凋亡的mcl-1蛋白,3-硫吗啡啉8-氧代8H-Ac [1,2-B]吡咯9-腈(s1)的纳摩尔抑制剂.s1通过结合到mcl-1的bh3凹槽发挥其功能.基于这种空间结构特征,我们使用基于片段的药物发现方法开发了一类新型的mcl-1抑制剂.通过解剖s1,我们鉴定出具有2-羟基吡啶核的化合物4为起始片段.在随后的分子生长中,我们使用了配体效率评估和拟合质量得分来评估片段.新型有效化合物n-苄基-5-(4-异丙基硫代苯酚)-2-羟基烟酰胺(12C),获得结合mcl-1的ic 50值为54 Nm.化合物12C显示出比s1更好的水溶性.
DOI:10.1016/j.Ejmech.2012.12.016

专利信息

专利号:US-2025026766-A1
优先权日:2022-01-12
标题 :Thiazolopyridyl Amide Derivatives as DNA Polymerase Theta Inhibitors
发明人：LI JING; XU WENQING; WANG ZHIWEI
权利人:BEIGENE LTD
摘要:The present invention relates to compounds containing thiazolopyridyl amide structure, the process for their synthesis, as well as the use of such compounds for inhibiting DNA Polymerase Theta (Pol Theta), and in the treatment of various diseases including cancers.