Background: Flt3 is an oncogenic kinase involved in different leukemias. It is most prominently associated with acute myeloid leukemia (AML). Flt3-specific inhibitors have shown promising results in interfering with AML.

Methods: The crystallographic structures of two inhibitors complexed within Flt3, namely, quizartinib and F6M, were used to guide the synthesis of new sulfonamide-based Flt3 inhibitors.

Results: One of the prepared compounds showed low micromolar anti-Flt3 bioactivity, and interestingly, low micromolar bioactivity against the related oncogenic kinase VEGFR2.

Conclusion: Sulfonamides were successfully used as privileged scaffolds for the synthesis of novel Flt3 inhibitors of micromolar potencies.

背景：Flt3是一种涉及不同白血病的致癌激酶。它与急性髓细胞性白血病（AML）最明显相关。Flt3特异性抑制剂在干扰AML方面显示出令人鼓舞的结果。

方法：使用两种在Flt3中复合的抑制剂，即quizartinib和F6M的晶体学结构，指导新的基于磺酰胺的Flt3抑制剂的合成。

结果：制备的化合物之一显示出低的微摩尔抗Flt3生物活性，并且有趣的是，其对相关的致癌激酶VEGFR2的低微摩尔生物活性。

结论：磺酰胺已成功地用作特权支架，用于合成新型的Flt3微摩尔效价抑制剂。