864461-13-2Relevant articles and documents
Discovery of BAY-985, a Highly Selective TBK1/IKK? Inhibitor
Lefranc, Julien,Schulze, Volker Klaus,Hillig, Roman Christian,Briem, Hans,Prinz, Florian,Mengel, Anne,Heinrich, Tobias,Balint, Jozsef,Rengachari, Srinivasan,Irlbacher, Horst,St?ckigt, Detlef,B?mer, Ulf,Bader, Benjamin,Gradl, Stefan Nikolaus,Nising, Carl Friedrich,Von Nussbaum, Franz,Mumberg, Dominik,Panne, Daniel,Wengner, Antje Margret
supporting information, p. 601 - 612 (2020/02/04)
The serine/threonine kinase TBK1 (TANK-binding kinase 1) and its homologue IKK? are noncanonical members of the inhibitor of the nuclear factor κB (IκB) kinase family. These kinases play important roles in multiple cellular pathways and, in particular, in inflammation. Herein, we describe our investigations on a family of benzimidazoles and the identification of the potent and highly selective TBK1/IKK? inhibitor BAY-985. BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 and displays antiproliferative efficacy in the melanoma cell line SK-MEL-2 but showed only weak antitumor activity in the SK-MEL-2 human melanoma xenograft model.
NOVEL CYCLIC COMPOUND HAVING 4-PYRIDYLALKYLTHIO GROUP HAVING (UN)SUBSTITUTED AMINO INTRODUCED THEREIN
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Page/Page column 37-38, (2008/06/13)
A novel cyclic compound having a 4-pyridylalkylthio group having an (un) substituted amino group introduced therein or a salt thereof. They are useful as a medicine. The cyclic compound is a compound represented by the following formula (1), which is useful for the treatment of diseases in which angiogenesis participates. In the following formula (1), ring A represents a benzene ring or a 5- or 6-membered aromatic heterocycle optionally fused with a cycloalkane ring; B represents alkylene; R1 and R2 each represents H, (substituted) aryl, (substituted) heterocyclic group, etc.; R3 and R4 each represents H; (substituted) alkyl, (substituted) cycloalkyl, -Z-R5, etc.; R5 represents (substituted) alkyl, (substituted) aryl, (substituted) heterocyclic group, etc.; X and Y each represents H, etc.; Z represents -CO-, -COO-, -CONR 6- -SO2-, etc.; R6 represents H, etc.; p is 0, 1, or 2; and q is 0 or 1.