Table 5 Benzimidazole-based FLT3 inhibitors

Target

FLT3, and PDGFR α/ẞ

[80, 81, 108, 109]

Binding mode to FLT3 kinase

Type I

Mutation point

F691L

FLT3 Potency (IC₅₀)

2, 1.3, 2 nM (FLT3-ITD (in MV4-16and MOLM 15), FLT3-ITD (in Ba/F3 cells), FLT3-wt (in SEMK2 cells))

In vitro targeted AML cells (IC₅₀)

1.3 and 4.9 nM (in MV4-16, and MOLM 18, respectively)

Target

FLT3

[111]

Binding mode to FLT3 kinase

Type I

FLT3 Potency (IC₅₀)

495 nM

Target

FLT3-wt, FLT3-ITD, and FLT-TKD-D835Y

[112]

Binding mode to FLT3 kinase

Type I

FLT3 Potency (IC₅₀)

43.8, 97.2, and 92.5 nM, respectively

In vitro targeted AML cells (IC₅₀)

38.8 and 54.9 nM (in MV4-16 (expressing FLT3-ITD), and MOLM-18(expressing FLT3-ITD), respectively)