Zhang, Qing published the artcileSynthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors, Related Products of catalysis-chemistry, the publication is Bioorganic & Medicinal Chemistry Letters (2020), 30(23), 127525, database is CAplus and MEDLINE.
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.
Bioorganic & Medicinal Chemistry Letters published new progress about 104-03-0. 104-03-0 belongs to catalysis-chemistry, auxiliary class Nitro Compound,Carboxylic acid,Benzene, name is 4-Nitrophenylacetic acid, and the molecular formula is C5H6BNO2, Related Products of catalysis-chemistry.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia