1083326-23-1Relevant articles and documents
Identification of novel thiazolo[5,4-b]pyridine derivatives as potent phosphoinositide 3-kinase inhibitors
Dong, Yi,Lin, Songwen,Tian, Hua,Xia, Liang,Xu, Heng,Zhang, Jingbo,Zhang, Kehui,Zhang, Yan
, (2020)
A series of novel 2-pyridyl, 4-morpholinyl substituted thiazolo[5,4-b]pyridine analogues have been designed and synthesized in this paper. These thiazolo[5,4-b]pyridines were efficiently prepared in seven steps from commercially available substances in mo
Benzenesulphonamide inhibitors of the cytolytic protein perforin
Spicer, Julie A.,Miller, Christian K.,O'Connor, Patrick D.,Jose, Jiney,Huttunen, Kristiina M.,Jaiswal, Jagdish K.,Denny, William A.,Akhlaghi, Hedieh,Browne, Kylie A.,Trapani, Joseph A.
supporting information, p. 1050 - 1054 (2017/09/30)
The pore-forming protein perforin is a key component of mammalian cell-mediated immunity and essential to the pathway that allows elimination of virus-infected and transformed cells. Perforin activity has also been implicated in certain auto-immune conditions and therapy-induced conditions such as allograft rejection and graft versus host disease. An inhibitor of perforin activity could be used as a highly specific immunosuppressive treatment for these conditions, with reduced side-effects compared to currently accepted therapies. Previously identified first-in-class inhibitors based on a 2-thioxoimidazolidin-4-one core show suboptimal physicochemical properties and toxicity toward the natural killer (NK) cells that secrete perforin in vivo. The current benzenesulphonamide-based series delivers a non-toxic bioisosteric replacement possessing improved solubility.
PYRIDOPYRIMIDINE DERIVATIVES AS PI3 KINASE INHIBITORS
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Page/Page column 51, (2009/04/25)
Invented is a method of inhibiting the activity/function of PB kinases using pyridoprimidine derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of pyridopyrimidine derivatives.