Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595431 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
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 (e.g., 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 EC50 reached 14Â nM.
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Authors
Zhijie Wu, Ying Li, Yu Cai, Junying Yuan, Chengye Yuan,