CAS: 28860-09-5; N-Ethyl-3-Nitrobenzenesulfonamide

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CAS号75-04-7 乙胺 | CAS号121-51-7 3-硝基苯磺酰氯 | CAS号56445-08-0 N-乙基-3-氨基苯磺酰胺

📜乙胺,3-硝基苯磺酰氯 以 四氢呋喃 用作溶剂,化学反应 0.5H,以92%的收率获得n-乙基-3-硝基苯磺酰胺
参考文献:Synthesis And Biological Evaluation Of Naphthoquinone Analogs As A Novel Class Of Proteasome Inhibitors
标题:Synthesis And Biological Evaluation Of Naphthoquinone Analogs As A Novel Class Of Proteasome Inhibitors
摘要:Screening Of The Nci Diversity Set-1 Identified Pi-083 (Nsc-45382) A Proteasome Inhibitor Selective For Cancer Over Normal Cells. Focused Libraries Of Novel Compounds Based On Pi-083 Chloronaphthoquinone And Sulfonamide Moieties Were Synthesized To Gain A Better Understanding Of The Structure-Activity Relationship Responsible For Chymotrypsin-Like Proteasome Inhibitory Activity. This Led To The Demonstration That The Chloronaphthoquinone And The Sulfonamide Moieties Are Critical For Inhibitory Activity. The Pyridyl Group In Pi-083 Can Be Replaced With Other Heterocyclic Groups Without Significant Loss Of Activity. Molecular Modeling Studies Were Also Performed To Explore The Detailed Interactions Of Pi-083 And Its Derivatives With The Beta 5 And Beta 6 Subunits Of The 20S Proteasome. The Refined Model Showed An H-Bond Interaction Between The Asp-114 And The Sulfonamide Moiety Of The Pi-083 In The Beta 6 Subunit. (C) 2010 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmc.2010.06.038