期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 8, 期 4, 页码 407-412出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.6b00489
关键词
Apoptosis inhibitors; phenotypic screen; structure-activity optimization; ischemia treatment; mitochondria protection
资金
- National High Technology Project 973 [2011CB504300]
A series of 2-sulfonyl-pyrimidinyl derivatives was developed as apoptosis inhibitors. These represent the first class of apoptosis inhibitors that function through stabilizing mitochondrial respiratory complex II. Starting from a phenotypic screen hit with micromolar activity, we optimized the cellular apoptosis inhibition activity of 2-sulfonyl-pyrimidinyl derivatives to picomolar level (compound 42, also named as TC9-305). The therapeutic potential of these new apoptosis inhibitors was further demonstrated by their neuroprotective effect on an ischemic animal model.
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