doi: 10.1016/j.bmcl.2013.06.073.
Epub 2013 Jul 3.
A novel necroptosis inhibitor-necrostatin-21 and its SAR study
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- PMID: 23886688
- DOI: 10.1016/j.bmcl.2013.06.073
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A novel necroptosis inhibitor-necrostatin-21 and its SAR study
Bioorg Med Chem Lett.
.
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 17 b was 35-fold as potent as the lead, while EC50 reached 14 nM.
Keywords: Inhibitor; JNK3; Nec-21; Necroptosis; RIP1; SAR study.
Copyright © 2013 Elsevier Ltd. All rights reserved.
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