CAS: 159013-94-2; Methyl 4-Amino-1,2,5-Oxadiazole-3-Carboxylate

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78350-50-2 17376-63-5 1092310-34-3

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CAS号67-56-1 甲醇 | CAS号78350-50-2 3-氨基呋咱-4-羧酸

📜3-氨基呋咱-4-羧酸置于盐酸体系中,用 甲醇 用作溶剂,化学反应 8.0H,以91%的收率获得4-氨基-1,2,5-恶二唑-3-羧酸甲酯
参考文献:Discovery Of Selective Small-Molecule Inhibitors For The β-Catenin/t-Cell Factor Protein-protein Interaction Through The Optimization Of The Acyl Hydrazone Moiety
标题:Discovery Of Selective Small-Molecule Inhibitors For The β-Catenin/t-Cell Factor Protein-protein Interaction Through The Optimization Of The Acyl Hydrazone Moiety
摘要:Acyl Hydrazone Is An Important Functional Group For The Discovery Of Bioactive Small Molecules. This Functional Group Is Also Recognized As A Pan Assay Interference Structure. In This Study,A New Small-Molecule Inhibitor For The Beta-Catenin/tcf Protein-Protein Interaction (Ppi),Zinc02092166,Was Identified Through Alphascreen And Fp Assays. This Compound Contains An Acyl Hydrazone Group And Exhibits Higher Inhibitory Activities In Cell-Based Assays Than Biochemical Assays. Inhibitor Optimization Resulted In Chemically Stable Derivatives That Disrupt The Beta-Catenin/tcf Ppi. The Binding Mode Of New Inhibitors Was Characterized By Site-Directed Mutagenesis And Structure-Activity Relationship Studies. This Series Of Inhibitors With A New Scaffold Exhibits Dual Selectivity For Beta-Catenin/tcf Over Beta-Catenin/cadherin And Beta-Catenin/apc Ppis. One Derivative Of This Series Suppresses Canonical Wnt Signaling,Downregulates The Expression Of Wnt Target Genes,And Inhibits The Growth Of Cancer Cells. This Compound Represents A Solid Starting Point For The Development Of Potent And Selective Beta-Catenin/tcf Inhibitors.
Doi:10.1021/acs.Jmedchem.5B00223