CAS: 56766-13-3; 4-(3-Oxobutanamido)Benzamide

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4-aminobenzamide ethyl acetoacetate .I. pigment yellow 12C.I. pigment yellow 12

📜对氨基苯甲酰胺,乙酰乙酸乙酯置于potassium Tert-Butylate体系中,化学反应 2.0H,反应生成 4-甲酰氨基-N-乙酰乙酰苯胺
参考文献:Discovery And Optimization Of Novel,Selective Histone Methyltransferase Set7 Inhibitors By Pharmacophore-And Docking-Based Virtual Screening
标题:Discovery And Optimization Of Novel,Selective Histone Methyltransferase Set7 Inhibitors By Pharmacophore-And Docking-Based Virtual Screening
摘要:Histone Methyltransferases Are Involved In Various Biological Functions,And These Methylation Regulating Enzymes' Abnormal Expression Or Activity Has Been Noted In Several Human Cancers. Within This Context,Set Domain-Containing (Lysine Methyltransferase) 7 (Set7,Also Called Kmt7,Setd7,Set9) Is Of Increasing Significance Due To Its Diverse Roles In Biological Functions And Diseases,Such As Diabetes,Cancers,Alopecia Areata,Atherosclerotic Vascular Disease,Hiv,And Hcv. In This Study,Dc-S100,Which Was Discovered By Pharmacophore-And Docking-Based Virtual Screening,Was Identified As The Hit Compound Of Set7 Inhibitor. Structure-Activity Relationship (Sar) Analysis Was Performed On Analogs Of Dc-S100 And According To The Putative Binding Mode Of Dc-S100,Structure Modifications Were Made To Improve Its Activity. Of Note,Compounds Dc-S238 And Dc-S239,With Ic50 Values Of 4.88 And 4.59 Mu M,Respectively,Displayed Selectivity For Dnmt1,Dot1L,Ezh2,Nsd1,Setd8,And G9A. Taken Together,Dc-S238 And Dc-S239 Can Serve As Leads For Further Investigation As Set7 Inhibitors And The Chemical Toolkits For Functional Biology Studies Of Set7.
DOI:10.1021/acs.Jmedchem.5B01154