Table 7. β-Fluorinated Analogues of 4-Methoxytriphenylbutanamine 26.
compd | R1 | R2 | pKa | inhibition of basal ATPase activity Kiapp (nM) | LE | K562 cells GI50 (nM) |
---|---|---|---|---|---|---|
26 | H | H | 9.86 ± 0.05 | 15.5 ± 5.3 | 0.43 | 83 ± 4 |
rac-52 | F | H | 7.86 ± 0.07 | 27.3 ± 1.2 | 0.40 | 652 ± 61 |
53 | F2 | H | 7.11 ± 0.05 | 88.4 ± 1.9 | 0.36 | 2624 ± 379 |
rac-54 | H | CF3 | 4.63 ± 0.10 | 2268 ± 39 | 0.27 | >100000 |