Table 2. SAR (Continued)a.
IC50 (nM) |
|||||||
---|---|---|---|---|---|---|---|
compd | R1 | R2 | MW | LE | TNKS1 FP | TNKS2 FP | β-cat luc |
20 | H | H | 485.5 | 0.32 | 7.9 | 79.4 | 63.1 |
21 | CH3 | H | 499.5 | 0.32 | 4.0 | 63.1 | 20.0 |
22 | OCH3 | H | 515.5 | 0.30 | 8.1 | 125.9 | 20.0 |
23 | F | H | 503.5 | 0.28 | 39.8 | 316.2 | 63.1 |
24 | Cl | H | 519.9 | 0.30 | 15.8 | 125.9 | 63.1 |
25 | CH3 | F | 517.4 | 0.30 | 6.3 | 79.4 | 20.0 |
26 | CH3 | CH3 | 513.5 | 0.29 | 15.8 | 79.4 | 251.2 |
The values are the geometric mean of at least two determinations. All individual values are within 25% of the mean.