Table 1.

SAR of all the targeted compounds for anti-HCV activity in Huh7.5 cells

Code	R1	R2	CC50 (μM)a	EC50 (μM)b	SI
1	C6H4OCH3-4	COOH	> 1000	43.8 ± 3.81	> 22.8
2	C6H4F-4	COOCH3	274 ± 8.35	2.09 ± 1.65	131
3a	C6H4F-4	CH2OH	285 ± 7.45	2.99 ± 1.51	95.3
3b	CH2CH2CH3	CH2OH	> 500	16.4 ± 10.9	> 30.5
3c	CH2(CH2)5CH3	CH2OH	33.3 ± 6.49	1.01 ± 0.55	32.9
3d	CH2(CH2)6CH3	CH2OH	17.8 ± 2.44	0.80 ± 0.26	22.3
6a	C6H4OCH3-4	COOCH3	414 ± 7.34	7.01 ± 1.51	59.1
6b	C6H4CH3-4	COOCH3	132.9 ± 7.53	1.73 ± 1.36	76.8
6c	C6H4CH = CH2-4	COOCH3	81.2 ± 12.9	1.61 ± 0.76	50.4
6d	C6H3F2-2,4	COOCH3	261 ± 28.7	1.69 ± 1.47	154
6e	C6H4NO2-4	COOCH3	235 ± 48.2	14.2 ± 3.13	16.5
6f	pyridyl-4	COOCH3	> 500	4.66 ± 0.35	> 107
7a	C6H4OCH3-4	CH2OH	383 ± 30.2	2.81 ± 0.82	136
7b	C6H4CH3-4	CH2OH	252 ± 3.04	< 2.06	> 122
7c	C6H4CH = CH2-4	CH2OH	143 ± 32.3	3.16 ± 0.51	45.3
7d	C6H3F2-2,4	CH2OH	266 ± 9.47	< 2.06	> 129
7e	Pyrid-4-yl	CH2OH	> 500	9.03 ± 5.58	> 55.4
7f	Pyrid-3-yl	CH2OH	> 500	4.39 ± 3.01	> 114
7 g	pyrid-2-ylCl-5	CH2OH	> 500	10.9 ± 5.59	> 45.9
7 h	CONHC6H4	CH2OH	> 500	46.7 ± 41.0	> 10.7
7i	CONHC6H3CF3-4	CH2OH	86.2 ± 4.33	4.19 ± 1.44	20.6
9			41.9 ± 1.10	1.16 ± 0.25	36.1
10a	C6H4OCH3-4	CH3	> 140 ± 16.6	11.7 ± 0.06	12.0
10b	C6H4CH3-4	CH3	55.7 ± 7.50	0.82 ± 0.26	67.9
10c	C6H4CH3-4	C2H5	12.3 ± 4.23	< 0.23	> 53.5
10d	C6H3F2-2,4	CH3	156 ± 37.9	6.55 ± 2.69	23.8
10e	Pyrid-4-yl	CH3	> 500	80.4 ± 24.3	6.22
13a	4-OCH3	COOCH3	326 ± 21.0	16.7 ± 4.71	19.5
13b	4-F	COOCH3	260 ± 84.8	18.1 ± 6.49	14.4
13c	3-NO2	COOCH3	402 ± 83.6	40.4 ± 3.64	10.0
14a	4-OCH3	CH2OH	214 ± 95.0	8.80 ± 2.15	24.3
14b	4-F	CH2OH	156 ± 65.8	13.6 ± 2.63	11.5
20	3-NO2	CH2OH	312 ± 31.1	18.4 ± 1.64	17.0
Tela			47.6 ± 0.61	0.02 ± 0.02	1950

Tela telaprevir

^aCytotoxic concentration required to inhibit Huh7.5 cell growth by 50%

^bConcentration required to inhibit HCV growth by 50%