Table 1 In-vitro inhibition of FLT3 kinase by pyrimidine series of compounds 13a-13j and urea derivative 24a-b.
| |||||
|---|---|---|---|---|---|
Entry | R1 | R2 | X | FLT3a IC50 (nM) ± SD | LE |
13a | -Ph(4-SO2Me) | -Me | NH | 13.9 ± 6.5 | 0.28 |
13b | -Me | -Me | NH | 37.5 ± 13 | 0.35 |
13c |
| -Me | NH | 129.3 ± 0.9 | 0.26 |
13d |
| -Me | NH | 377 ± 20 | 0.24 |
13e | -Ph(4-SO2Me) | -Me | O | 267.6 ± 25 | 0.24 |
13f | -Ph(3-CF3) | -Me | O | 961 ± 33.7 | 0.22 |
13g | -Ph(4-SO2Me) | -Ph(4-F) | NH | 3225 ± 556 | 0.17 |
13h | -Ph(4-SO2Me) | -Ph(4-Me) | NH | 4842 ± 170 | 0.16 |
13i | Morpholine | -Me | NH | 428 ± 99 | 0.27 |
13j | 1-methylpiperazine | -Ph(4-Br) | NH | 6024 ± 122 | 0.18 |
24a | -Ph(4-SO2Me) | -Me | NH | 41 ± 6.8 | 0.27 |
24b | -Me | -Me | NH | 38.2 ± 1.5 | 0.37 |
