Table 5.
IC50 ChoK and HT-29 values for the bisquinolinium derivatives belonging to series B.
| ||||
|---|---|---|---|---|
| Comp. | Linker | R4 | (IC50)ex vivo (μM) a,b |
(IC50)HT-29 (μM) a,c |
| 43 | Biphenyl-3,3′-diyl | Amino | 20.6 | 1.90 |
| 44 | Dimethylamino | 9.60 | 0.70 | |
| 45 | Pyrrolidino | 1.20 | 0.40 | |
| 46 | N-Methylanilino | 3.10 | 1.00 | |
| 47 | 4-Chloro-N-methylanilino | 5.70 | 1.90 | |
| 48 | Biphenyl-4,4′-diyl | Amino | 63.3 | 3.20 |
| 49 | Dimethylamino | 20.6 | 0.80 | |
| 50 | Pyrrolidino | 19.8 | 2.40 | |
| 51 | N-Methylanilino | 11.4 | 0.50 | |
| 52, RSM-932A | 4-Chloro-N-methylanilino | 11.4 | 1.20 | |
| 53 | Bibenzyl-4,4′-diyl | Amino | 80.0 | 2.00 |
| 54 | Dimethylamino | 9.00 | 0.27 | |
| 55 | Pyrrolidino | 1.00 | 0.20 | |
| 56 | N-Methylanilino | 3.50 | 0.50 | |
| 57 | 4-Chloro-N-methylanilino | 5.70 | 0.80 | |
a All values are the mean of two independent determinations performed in duplicate. b Recombinant human ChoK was used as a target. c in vitro assay carried out on the HT-29 cell line.