Table 1. Structures and Ki Values of 5- or 6-Substituted Compounds against IDH1(R132H).
R5 | R6 | Ki (μM) | |
---|---|---|---|
5 | -Ph | -H | ∼50 |
4 | -Bn | -H | 8.2 |
10 | -(CH2)2Ph | -H | >50 |
11 | -(CH2)3Ph | -H | >50 |
6 | -OPh | -H | 46 |
12 | -CONHOH | -H | >50 |
13 | -CONHBn | -H | >50 |
14 | -NHCOBn | -H | >50 |
15 | -H | -Ph | >50 |
7 | -H | -Bn | 5.9 |
16 | -H | –CH(CH3)Ph | >50 |
17 | -H | -(CH2)2Ph | 10 |
18 | -H | -(CH2)2(4-CO2Me-Ph) | 27 |
8 | -H | -CONHOH | 4.5 |