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.

作为III类受体酪氨酸激酶（RTK），FMS样酪氨酸激酶3（FLT3）在许多急性白血病病例中总是过表达。本文研究了二芳基脲衍生物作为FLT3抑制剂的结构化合成和生物学评价。令人鼓舞的是，化合物15b，16b，24a和24c在低纳摩尔范围内显示出出色的生物活性。特别地，化合物16b表现出对FLT3-ITD的显着抑制作用（IC ₅₀＝ 5.60nM），并且比奎扎替尼对MV4-11细胞系具有更好的抗增殖活性（IC ₅₀＝0.176nM ）。表明化合物16b 对于急性髓细胞白血病的治疗可能非常有前途。