Structure–activity relationship study of novel necroptosis inhibitors

X Teng, A Degterev, P Jagtap, X Xing, S Choi…

文献索引：Teng, Xin; Degterev, Alexei; Jagtap, Prakash; Xing, Xuechao; Choi, Sungwoon; Denu, Regine; Yuan, Junying; Cuny, Gregory D. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 22 p. 5039 - 5044

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被引用次数: 114

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-α. 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 ...