. 2021 May 25;13(6):788. doi: 10.3390/pharmaceutics13060788

Table 4.

IC₅₀ ChoK and HT-29 values for the bisquinolinium derivatives belonging to series A.


Comp.	Linker	R³	R⁴	(IC₅₀)_{ex vivo} (μM) ^a,b	(IC₅₀)_HT-29 (μM) ^a,c
23	Biphenyl-3,3′-diyl	H	Amino	1.20	1.90
24		Me	Amino	11.9	4.40
25		H	Dimethylamino	4.40	1.60
26		H	Perhydroazepino	0.50	0.50
27		H	Anilino	1.30	1.60
28		H	N-Methylanilino	0.40	0.80
29		H	4-Chloro-N-methylanilino	2.10	1.50
30	Biphenyl-4,4′-diyl	H	Amino	81.1	2.20
31		Me	Amino	>200	3.30
32		H	Dimethylamino	39.7	1.70
33		H	Perhydroazepino	2.20	0.50
34		H	Anilino	17.8	0.70
35		H	N-Methylanilino	3.00	0.60
36		H	4-Chloro-N-methylanilino	2.00	1.20
37	Bibenzyl-4,4′-diyl	H	Amino	80.0	2.00
38		H	Dimethylamino	10.2	0.50
39		H	Perhydroazepino	0.60	0.30
40		H	Anilino	2.30	0.30
41		H	N-Methylanilino	1.40	0.70
42		H	4-Chloro-N-methylanilino	4.80	0.70

^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.