Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 17, Pages 4903-4906Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.06.073
Keywords
Necroptosis; Nec-21; Inhibitor; SAR study; RIP1; JNK3
Categories
Funding
- National Natural Science Foundation of China [21072212]
- National Institute of Health of US [R37 AG012859]
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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 14 nM. (C) 2013 Elsevier Ltd. All rights reserved.
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