Table 1.
Cholinesterase activity and cytotoxicity of the M2 bitopic compounds and tacrine hybrids. BChE from equine serum, AChE from electric eel. [110].
| Compound | BChE pIC50 [M] |
AChE pIC50 [M] |
Cytotoxicity HEP G2 IC50 [μM] |
|---|---|---|---|
| Tacrine (42) | 8.57 | 7.60 | 111 (±2.28) |
| Phth-7-iper (5a-C7) | 5.19 | 4.83 | n.d. 1 |
| Phth-8-iper (5a-C8) | 5.13 | 4.89 | n.d. 1 |
| Phth-9-iper (5a-C9) | 4.88 | 4.80 | n.d. 1 |
| Phth-10-iper (5a-C10) | 5.37 | 5.26 | n.d. 1 |
| Naph-7-iper (5b-C7) | 6.69 | 6.04 | n.d. 1 |
| Naph-8-iper (5b-C8) | 6.46 | 6.10 | n.d. 1 |
| Naph-9-iper (5b-C9) | 6.49 | 6.44 | n.d. 1 |
| Naph-10-iper (5b-C10) | 6.99 | 6.50 | n.d. 1 |
| Tac-7-Tac (43-C7) | 9.14 | 10.48 | <1.38 (±0.08) |
| Tac-10-Tac (43-C10) | 9.34 | 9.00 | <1.25 (±0.00) |
| Phth-4-isoxo (44-C4) | 4.07 | 19.12% inhib. at 100 μM | n.d. 1 |
| Phth-6-isoxo (44-C6) | 4.41 | 32.91% inhib. at 100 μM | n.d. 1 |
| Phtal-8-isoxo (44-C8) | 5.10 | 4.17 | n.d. 1 |
| Tac-7-iper (45-C7) | 8.29 | 8.76 | >160 (±0.00) |
| Tac-10-iper (45-C10) | 8.75 | 9.81 | 32.2 (±0.41) |
1 n.d.: not determined.