Discovery and optimization of a highly efficacious class of 5-aryl-2-aminopyridines as FMS-like tyrosine kinase 3 (FLT3) inhibitors was written by Liu, Gang;Abraham, Sunny;Liu, Xing;Xu, Shimin;Rooks, Allison M.;Nepomuceno, Ron;Dao, Alan;Brigham, Daniel;Gitnick, Dana;Insko, Darren E.;Gardner, Michael F.;Zarrinkar, Patrick P.;Christopher, Ron;Belli, Barbara;Armstrong, Robert C.;Holladay, Mark W.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2015.SDS of cas: 59669-59-9 This article mentions the following:
Based on a putative binding mode of quizartinib, a potent FMS-like tyrosine kinase 3 (FLT3) inhibitor in Phase III clin. development, the authors have designed de novo a simpler aminopyridine-based hinge binding motif. Further optimization focusing on maximizing in vivo efficacy and minimizing CYP3A4 time-dependent inhibition resulted in a highly efficacious compound I in tumor xenograft model for further preclin. development. In the experiment, the researchers used many compounds, for example, 3-(tert-Butyl)isoxazol-5-amine (cas: 59669-59-9SDS of cas: 59669-59-9).
3-(tert-Butyl)isoxazol-5-amine (cas: 59669-59-9) belongs to isoxazole derivatives. Isoxazoles also form the basis for a number of drugs, including the COX-2 inhibitor valdecoxib (Bextra) and a neurotransmitter agonist AMPA. The most common methods for N–O bond cleavage in isoxazoles are hydrogenation with palladium or platinum catalysts or with Raney Ni. Recent developments have shown that Mo(CO)6 efficiently cleaves the N–O bond in isoxazoles.SDS of cas: 59669-59-9
Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem