Targeting Wnt/β-catenin pathway in hepatocellular carcinoma treatment

Table 2 Percentage inhibition of [³H]-thymidine incorporation in Huh-7 cells by FH535 analogs

FH535 analog	C-2	C-3	C-4	C-5	C-6	C-2'	C-3'	C-4'	C-5'	C-6'	[3H]-Thymidine incorporation ratio in Huh-7 cells at 10μmol/L relative to DMSO	% Inhibition at 10μmol/L	Ratio of % inhibition of analog to % inhibition by FH535 at 10μmol/L	TOPFlash Assay (10μmol/L)	TOPFlash Assay as a Percentage Decrease Relative to Control
Control											100 ± 10			31.2 ± 4.5
1a	Cl	H	H	Cl	H	CH3	H	NO2	H	H	64 ± 3.7	36	1.0	8.5 ± 2.1	73
1b	Cl	H	H	Cl	H	CH3	H	CO2CH3	H	H	82 ± 4.2	18	0.5
1c	Cl	H	H	Cl	H	CO2CH3	H	F	H	H	93 ± 5.6	7	0.2	12.1 ± 0.9	61
1d	Cl	H	H	Cl	H	CO2CH3	H	Cl	H	H	106 ± 14	0	0.0
1e	Cl	H	H	Cl	H	CH3	H	CH2OH	H	H	33 ± 4.8	67	1.9
1f	Cl	H	H	Cl	H	1-(4-NO2)C10H6					52 ± 6.4	48	1.3
1g	Cl	H	H	H	Cl	CH3	H	CO2CH3	H	H	71 ± 1	29	0.8
1h	Cl	H	H	H	Cl	CH3	H	CH2OH	H	H	27 ± 5.1	73	2.0	27.3 ± 3.5	13
1i	F	H	H	H	F	CH3	H	CH2OH	H	H	62 ± 1.5	38	1.1
1j	H	H	H	H	H	CH3	H	CH2OH	H	H	47 ± 2.3	53	1.5
1k	F	H	H	H	F	OC6H5	H	H	H	H	66 ± 3.2	34	0.9
1l	F	H	H	H	F	H	OCH2C6H5	H	H	H	57 ± 21	43	1.2
1m	Cl	H	H	H	Cl	H	H	COC6H5	H	H	67 ± 12	33	0.9
1n	F	H	H	F	H	1-(4-NO2)C10H6					69 ± 3.51	31	0.9	11.2 ± 1.0	64
1o	Cl	H	H	H	Cl	OC6H5	H	H	H	H	62 ± 10	38	1.1	17.2 ± 0.9	45
1p	Cl	H	H	H	Cl	H	OCH2C6H5	H	H	H	69 ± 6.9	31	0.9	14.8 ± 0.7	53
1q	F	H	H	H	F	H	H	COC6H5	H	H	67 ± 5.9	33	0.9
1r	Cl	H	H	H	Cl	1-(4-NO2)C10H6					74 ± 27	26	0.7	16.6 ± 1.1	47
1s	H	H	H	H	H	H	OCH2C6H5	H	H	H	71 ± 12	29	0.8
1t	H	H	H	H	H	H	H	COC6H5	H	H	62 ± 2.3	38	1.1	16.8 ± 0.9	46
1u	H	H	H	H	H	1-(4-NO2)C10H6					58 ± 6.9	42	1.2	8.7 ± 0.1	72

From Kril et al[70] with permission of Bioorg Med Chem Lett.