Structure–activity relationship study of [1, 2, 3] thiadiazole necroptosis inhibitors

…, H Keys, A Jeevanandam, JA Porco, A Degterev…

Index: Teng, Xin; Keys, Heather; Jeevanandam, Arumugasamy; Porco Jr., John A.; Degterev, Alexei; Yuan, Junying; Cuny, Gregory D. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 24 p. 6836 - 6840

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Citation Number: 42

Abstract

Necroptosis is a regulated caspase-independent cell death mechanism that results in morphological features resembling non-regulated necrosis. This form of cell death can be induced in an array of cell types in apoptotic deficient conditions with death receptor family ligands. A series of [1, 2, 3] thiadiazole benzylamides was found to be potent necroptosis inhibitors (called necrostatins). A structure–activity relationship study revealed that small ...