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Relevant academic research and scientific papers

Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors

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.

Benzo imidazo [2, 1-b] thiazole compound and application thereof (by machine translation)

The invention discloses a benzoimidazo [2, 1-b] thiazole compound and application thereof, and belongs to the technical field of medicines. The inhibitory activity of the synthesized benzimidazo [2, 1-b] thiazole analogues on FLTT3 is more than 90%, wherein the compounds (compounds 2 , 4, 6, 8 and 10) are IC of FLTT3-ITD kinase. 50 Lower value, in particular compound 2, IC IC50 The value is only 5.60 nm, and therefore the compound of the present invention may be used as an inhibitor FLTT3, or for preparing a drug capable of modulating or suppressing diseases associated with abnormal cell proliferation by affecting the enzymatic activity of one or more tyrosine kinases and interfering with aberrant cell proliferation, having a wide application prospect. (by machine translation)

UREA DERIVATIVES AS KINASE MODULATORS

The invention provides methods and compositions for treating conditions mediated by various kinases wherein derivatives of urea compounds are employed. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.