433958-64-6Relevant articles and documents
Cu(OAc)2/DABCO-mediated domino reaction of vinyl malononitriles with cyclic sulfamidate imines: access to 6-hydroxyaryl-2-aminonicotinonitriles
Goud, S Banuprakash,Guin, Soumitra,Prakash, Meher,Samanta, Sampak
, p. 352 - 357 (2022/01/20)
A novel Cu(ii)–salt/DABCO-mediated one-pot access to a myriad of highly substituted biologically relevant 2-aminonicotinonitriles possessing a resourceful phenolic moiety with satisfactory yields is reported. This method involves cyclic sulfamidate imines as 1C1N sources and different kinds of acyclic/cyclic vinyl malononitriles as 4C sources for pyridine synthesis via a vinylogous Mannich-cycloaromatization sequence process, creating two new C–N bonds under mild conditions. Importantly, this de novo strategy is applicable to gram-scale syntheses, underlining the method's practicability and allowing for a wide range of substrates with excellent functional group tolerance.
Discovery of novel and selective IKK-β serine-threonine protein kinase inhibitors. Part 1
Murata, Toshiki,Shimada, Mitsuyuki,Sakakibara, Sachiko,Yoshino, Takashi,Kadono, Hiroshi,Masuda, Tsutomu,Shimazaki, Makoto,Shintani, Takuya,Fuchikami, Kinji,Sakai, Katsuya,Inbe, Hisayo,Takeshita, Keisuke,Niki, Toshiro,Umeda, Masaomi,Bacon, Kevin B.,Ziegelbauer, Karl B.,Lowinger, Timothy B.
, p. 913 - 918 (2007/10/03)
IκB kinase β (IKK-β) is a serine-threonine protein kinase critically involved in the activation of the transcription factor Nuclear Factor kappa B (NF-κB) in response to various inflammatory stimuli. We have identified a small molecule inhibitor of IKK-β. Optimization of the lead compound resulted in improvements in both in vitro and in vivo potency, and provided IKK-β inhibitors exhibiting potent activity in an acute cytokine release model (LPS-induced TNFα).