Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors was written by Zhang, Qing;Zhao, Kuantao;Zhang, Lixun;Jiao, Xiaoyu;Zhang, Yongjie;Tang, Chunlei. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2020.Quality Control of 3-(tert-Butyl)isoxazol-5-amine This article mentions the following:
As a class III receptor tyrosine kinase (RTK), FMS-like tyrosine kinase 3 (FLT3) is always overexpressed in many cases of acute leukemia. This paper studies the structure-based synthesis and biol. evaluation of diaryl urea derivatives as FLT3 inhibitors. Encouragingly, compounds 1-(3-(tert-butyl)isoxazol-5-yl)-3-(4-(7-methoxybenzo[d]imidazo[2,1-b]thiazol-2-yl)phenyl)urea , 1-(3-(tert-butyl)isoxazol-5-yl)-3-(4-(7-(2-morpholinoethoxy)benzo[d]imidazo[2,1-b]thiazol-2-yl)phenyl)urea , 1-(5-(tert-butyl)isoxazol-3-yl)-3-(2-(4-(2-morpholinoethoxy)phenyl)benzo[d]imidazo[2,1-b]thiazol-7-yl)urea , and 1-(3-(tert-butyl)isoxazol-5-yl)-3-(2-(4-(2-morpholinoethoxy)phenyl)benzo[d]imidazo[2,1-b]thiazol-7-yl)urea showed excellent biol. activities in a low nanomolar range. In particular, compound 1-(3-(tert-butyl)isoxazol-5-yl)-3-(4-(7-(2-morpholinoethoxy)benzo[d]imidazo[2,1-b]thiazol-2-yl)phenyl)urea demonstrated significant inhibitory potency against FLT3-ITD (IC50 = 5.60 nM) and better antiproliferative activity than quizartinib against MV4-11 cell line (IC50 = 0.176 nM). Compound 1-(3-(tert-butyl)isoxazol-5-yl)-3-(4-(7-(2-morpholinoethoxy)benzo[d]imidazo[2,1-b]thiazol-2-yl)phenyl)urea for the treatment of acute myeloid leukemia could be very promising. In the experiment, the researchers used many compounds, for example, 3-(tert-Butyl)isoxazol-5-amine (cas: 59669-59-9Quality Control of 3-(tert-Butyl)isoxazol-5-amine).
3-(tert-Butyl)isoxazol-5-amine (cas: 59669-59-9) belongs to isoxazole derivatives. Isoxazole are described as inhibitors of acetylcholinesterase (AChE). Isoxazole ligands bind to and inhibit the Sxc- antiporter. Some alternative routes for the synthesis of isoxazoles have also been developed and reported. The 2-benzoyl-2-halo-2H-azirines provide 4-haloisoxazoles in good yields after heating in toluene at reflux temperature.Quality Control of 3-(tert-Butyl)isoxazol-5-amine
Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem