Structure-activity relationship study of tricyclic 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-α. 5-(1-Indol-3-ylmethyl)-2-thiohydantoins and 5-(1-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.Graphical abstract
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关键词：
Necroptosis Caspase-independent cell death Stroke SAR Ischemic brain injury Indoles Hydantoin Central nervous system
DOI：
10.1016/j.bmcl.2005.07.077
被引量：
年份：
2005
Elsevier
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万方医学
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