A novel necroptosis inhibitor—necrostatin-21 and its SAR study

Z Wu, Y Li, Y Cai, J Yuan, C Yuan

文献索引：Wu, Zhijie; Li, Ying; Cai, Yu; Yuan, Junying; Yuan, Chengye Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 17 p. 4903 - 4906

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被引用次数: 13

摘要

Abstract An initial structure–activity relationship study of the novel necroptosis inhibitor Nec- 21 was described. Any changes of the tetracyclic scaffold were detrimental for the activity. Introduction of a substituent to 7 or 8 position (eg, cyano or methoxy group, respectively), would increase the activity. The 7 and 8-position disubstituted compound 17b was 35-fold as potent as the lead, while EC 50 reached 14 nM.