Table 1.
Overview of synthesised derivatives and their inhibition potency towards mIDH1 and wt IDH1/2.
| |||||
|---|---|---|---|---|---|
| IC50 (nM) a | |||||
| Compound | R | IDH1 R132H | IDH1 R132C | wt IDH1 | wt IDH2 |
| (S)-FT-2102 | Cl | 4.88 ± 1.63 | 178 ± 70 | >10,000 | >10,000 |
| (S)-2 | I | 5.23 ± 0.75 | 160 ± 24 | >10,000 | >10,000 |
| (R)-2 | I | 323 ± 83 | >10,000 | >10,000 | >10,000 |
| (S)-3 | F | 22.7 ± 5.2 | 579 ± 110 | >10,000 | >10,000 |
| (R)-3 | F | 698 ± 145 | >10,000 | >10,000 | >10,000 |
a Enzymatic IC50 values for mIDH1 and wt IDH1/2 are the mean of at least three determinations performed as described in Material and Methods (mean value ± standard deviation).