14192-58-6Relevant articles and documents
A novel necroptosis inhibitor - Necrostatin-21 and its SAR study
Wu, Zhijie,Li, Ying,Cai, Yu,Yuan, Junying,Yuan, Chengye
, p. 4903 - 4906 (2013/09/02)
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.
A pentacyclic aurora kinase inhibitor (AKI-001) with high in vivo potency and oral bioavailability
Rawson, Thomas E.,Rüth, Matthias,Blackwood, Elizabeth,Burdick, Dan,Corson, Laura,Dotson, Jenna,Drummond, Jason,Fields, Carter,Georges, Guy J.,Goller, Bernhard,Halladay, Jason,Hunsaker, Thomas,Kleinheinz, Tracy,Krell, Hans-Willi,Li, Jun,Liang, Jun,Limberg, Anja,McNutt, Angela,Moffat, John,Phillips, Gail,Ran, Yingqing,Safina, Brian,Ultsch, Mark,Walker, Leslie,Wiesmann, Christian,Zhang, Birong,Zhou, Aihe,Zhu, Bing-Yan,Rüger, Petra,Cochran, Andrea G.
scheme or table, p. 4465 - 4475 (2009/07/11)
Aurora kinase inhibitors have attracted a great deal of interest as a new class of antimitotic agents. We report a novel class of Aurora inhibitors based on a pentacyclic scaffold. A prototype pentacyclic inhibitor 32 (AKI-001) derived from two early lead
