Structure–activity relationship analysis of a novel necroptosis inhibitor, Necrostatin-5

K Wang, J Li, A Degterev, E Hsu, J Yuan…

Index: Wang, Ke; Li, Jinfeng; Degterev, Alexei; Hsu, Emily; Yuan, Junying; Yuan, Chengye Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 5 p. 1455 - 1465

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Citation Number: 56

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.