1079-47-6Relevant articles and documents
Protective Agent for Retinal Neuronal Cell Comprising Indazole Derivative as Active Ingredient
-
Page/Page column 8-9, (2009/01/23)
As a result of intensive studies for the purpose of finding a new medicinal use of an indazole derivative, it was found that an indazole derivative inhibits glutamate-induced retinal neuronal cell death in rat fetal retinal neuronal cells, in other words, the indazole derivative acts directly on the retinal neuronal cells and exhibits an effect of protecting retinal neuronal cells. Accordingly, the indazole derivative is useful for the prevention or treatment of an eye disease associated with retinal neuronal cell damage or retinal damage.
N-heterocyclic carbenes of 5-haloindazoles generated by decarboxylation of 5-haloindazolium-3-carboxylates
Schmidt, Andreas,Snovydovych, Bohdan,Habeck, Tobias,Droettboom, Petra,Gjikaj, Mimoza,Adam, Arnold
, p. 4909 - 4916 (2008/03/14)
Syntheses and properties of 5-fluoro-, chloro- bromo-, and iodo-substituted 11,2-dimethylindazohum-3-carboxylates as new representatives of pseudo-cross-conjugated heterocyclic mesomeric betaines are described, and results of an X-ray single crystal analy
Synthesis and SAR of indazole-pyridine based protein kinase B/Akt inhibitors
Woods, Keith W.,Fischer, John P.,Claiborne, Akiyo,Li, Tongmei,Thomas, Sheela A.,Zhu, Gui-Dong,Diebold, Robert B.,Liu, Xuesong,Shi, Yan,Klinghofer, Vered,Han, Edward K.,Guan, Ran,Magnone, Shayna R.,Johnson, Eric F.,Bouska, Jennifer J.,Olson, Amanda M.,Jong, Ron de,Oltersdorf, Tilman,Luo, Yan,Rosenberg, Saul H.,Giranda, Vincent L.,Li, Qun
, p. 6832 - 6846 (2007/10/03)
A series of heteroaryl-pyridine containing inhibitors of Akt are reported. The synthesis and structure-activity relationships are discussed, leading to the discovery of a indazole-pyridine analogue (Ki = 0.16 nM). These compounds bind in the ATP binding site, are potent, ATP competitive, and reversible inhibitors of Akt activity. No selectivity amongst the Akt isoforms is observed for this analogue, but there is good selectivity against an panel of other kinases. It is least selective for other members of the AGC family of kinases but is nonetheless 40-fold selective for Akt over PKA. The compound shows cellular activity and significantly slows tumor growth in vivo.
