📜6-溴-4-吲唑甲酸甲酯置于n-甲基吗啉,N-羟基-7-氮杂苯并三氮唑,1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物,Sodium Hydride,碳酸氢钠,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,Sodium Hydroxide体系中,用 四氢呋喃,1,4-二氧六环,甲醇,水,二甲基亚砜,N,N-二甲基甲酰胺 用作溶剂,化学反应 19.58H,反应生成N-((2-羟基-6-甲基-4-丙基-3-吡啶基)甲基)-1-异丙基-6-(2-(4-甲基-1-哌嗪基)-4-吡啶基)-1H-吲唑-4-甲酰胺
参考文献:Identification Of Potent,Selective,Cell-Active Inhibitors Of The Histone Lysine Methyltransferase Ezh2
标题:Identification Of Potent,Selective,Cell-Active Inhibitors Of The Histone Lysine Methyltransferase Ezh2
摘要:The Histone H3-Lysine 27 (H3K27) Methyltransferase Ezh2 Plays A Critical Role In Regulating Gene Expression,And Its Aberrant Activity Is Linked To The Onset And Progression Of Cancer. As Part Of A Drug Discovery Program Targeting Ezh2,We Have Identified Highly Potent,Selective,Sam-Competitive,And Cell-Active Ezh2 Inhibitors,Including Gsk926 (3) And Gsk343 (6). These Compounds Are Small Molecule Chemical Tools That Would Be Useful To Further Explore The Biology Of Ezh2.
Doi:10.1021/ml3003346