title: Structure-activity relationship analysis of a novel necroptosis inhibitor, Necrostatin-5.
abstract: Necrostatin-5 (Nec-5) is a novel potent small-molecule inhibitor of necroptosis structurally distinct from previously described Necrostatin-1 (Nec-1), and therefore, represents a new direction for the inhibition of this cellular caspase-independent necrotic cell death mechanism. Here, we describe a series of structural modifications of Nec-5 and the structure-activity relationship (SAR) of Nec-5 series in inhibiting necroptosis.
authors.affiliation: State Key Laboratory of Bio-organic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China.
authors.forename: Ke
authors.initials: K
authors.lastname: Wang
authors.forename: Jinfeng
authors.initials: J
authors.lastname: Li
authors.forename: Alexei
authors.initials: A
authors.lastname: Degterev
authors.forename: Emily
authors.initials: E
authors.lastname: Hsu
authors.forename: Junying
authors.initials: J
authors.lastname: Yuan
authors.forename: Chengye
authors.initials: C
authors.lastname: Yuan
mesh_terms: D017209:Apoptosis / Q000187:drug effects*; D006575:Heterocyclic Compounds, 3-Ring / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D019169:Jurkat Cells; D009336:Necrosis / Q000188:drug therapy*; D009570:Nitriles / Q000737:chemistry* / Q000494:pharmacology; D011744:Pyrimidinones / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013440:Sulfides / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D006575:Heterocyclic Compounds, 3-Ring; C519552:Necrostatin-5; D009570:Nitriles; D011744:Pyrimidinones; D013440:Sulfides