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参考文献:Structure-activity Relationship Study Of Novel Necroptosis Inhibitors
标题:Structure-activity Relationship Study Of Novel Necroptosis Inhibitors
摘要:Necroptosis Is A Regulated Caspase-Independent Cell Death Mechanism That Results In Morphological Features Resembling Necrosis. It Can Be Induced In A Fadd-Deficient Variant Of Human Jurkat T Cells Treated With Tnf-Alpha. 5-(1H-Indol-3-Ylmethyl)-2-Thiohydantoins And 5-(1H-Indol-3-Ylmethyl)Hydantoins Were Found To Be Potent Necroptosis Inhibitors (Called Necrostatins). A Sar Study Revealed That Several Positions Of The Indole Were Intolerant Of Substitution,While Small Substituents At The 7-Position Resulted In Increased Inhibitory Activity. The Hydantoin Ring Was Also Quite Sensitive To Structural Modifications. A Representative Member Of This Compound Class Demonstrated Moderate Pharmacokinetic Characteristics And Readily Entered The Central Nervous System Upon Intravenous Administration. (C) 2005 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmcl.2005.07.077