950769-61-6Relevant articles and documents
Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors
Jiao, Xiaoyu,Tang, Chunlei,Zhang, Lixun,Zhang, Qing,Zhang, Yongjie,Zhao, Kuantao
, (2020/10/02)
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 biological evaluation of diaryl urea derivatives as FLT3 inhibitors. Encouragingly, compounds 15b, 16b, 24a, and 24c showed excellent biological activities in a low nanomolar range. In particular, compound 16b 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). It is indicated that compound 16b for the treatment of acute myeloid leukemia could be very promising.
PROCESS FOR THE PREPARATION OF IMIDAZO[2,1-B][1,3]BENZOTHIAZOLE DERIVATIVES
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, (2011/06/11)
Provided herein are process for the preparation of N-(5-ferf-butyl-isoxazol-3-yl)- N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,l-fe][l,3]benzothiazol-2-yl]phenyl}urea, or a pharmaceutically acceptable salt, solvate, hydrate, or polymorph thereof. N-(5-tert- Butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,l-and][l,3]benzo- thiazol-2-yl]phenyl}urea is useful for treating, preventing, and/or managing diseases or conditions, including but not limited to, proliferative diseases, FLT-3 mediated diseases, and cancers. N-(5-ferf-Butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl- ethoxy)imidazo[2,l-and][l,3]benzothiazol-2-yl]phenyl}urea is represented by the structure:
IMIDAZOLOTHIAZOLE COMPOUNDS AS MODULATORS OF PROTEIN KINASE
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Page/Page column 78-79, (2010/06/11)
Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.