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. Author manuscript; available in PMC: 2013 Jul 15.
Published in final edited form as: Bioorg Med Chem Lett. 2012 May 24;22(14):4864–4868. doi: 10.1016/j.bmcl.2012.05.039

Table 1. Chemical Structure, Anti-HCV Activity and Cytotoxicity of Compounds 5-19.

graphic file with name nihms380374u1.jpg
Cmpd X X′ Y Y′ Z Z′ HCV Replicon (pM) Cytotoxicity, CC50 (μM)*
EC50 EC90 PBM CEM Vero
BMS-790052 H H H H H H 4.2 ± 1.5 20 ± 7.5 19 9.6 21
5b Cl Cl H H H H 6.4 ± 3.0 11.4 ± 4.8 2.8 12 ≥ 100
5a Br Br H H H H 5.9 ± 3.9 14 ± 8.3 2.9 5.7 84
5c I I H H H H 5.5 ± 1.9 11 ± 2.2 4.7 35 > 100
5d F F H H H H 6.8 ± 3.3 21.2 ± 11.0 19 3.0 > 100
5e H F H H H H 14.4 ±4.0 52.5 ±11.1 16 2.8 83
6 Ph Ph H H H H 200 700 > 100 37.4 > 100
7 graphic file with name nihms380374t1.jpg graphic file with name nihms380374t2.jpg H H H H 26 97 49.2 2.9 >100
8 graphic file with name nihms380374t3.jpg graphic file with name nihms380374t4.jpg H H H H 100 300 44.6 > 100 > 100
9 H H N3 N3 H H 23 35.2 20.3 18.4 > 100
10 H H H H N3 N3 18.4 ± 12.6 54.2 ± 34.1 > 100 ≥ 100 > 100
11 H H H H graphic file with name nihms380374t5.jpg graphic file with name nihms380374t6.jpg 2700 9200 > 100 > 100 > 100
12 H H H H graphic file with name nihms380374t7.jpg graphic file with name nihms380374t8.jpg 11.8 42.8 6.6 10.7 > 100
13 H H graphic file with name nihms380374t9.jpg graphic file with name nihms380374t10.jpg H H 757 102 > 104 96 > 100 > 100
14 H H graphic file with name nihms380374t11.jpg graphic file with name nihms380374t12.jpg H H > 104 > 104 > 100 > 100 > 100
15 Cl Cl H H N3 N3 4.7 9.6 7.8 3.8 > 100
16 Cl H H H N3 N3 6.3 29.5 9.7 31 > 100
17 Br Br H H N3 N3 2.6 21.6 19.8 10.8 > 100
18 Cl Cl N3 N3 H H 11.2 74.6 3.3 4.0 98.1
19 Br Br N3 N3 H H 8.3 55.3 3.4 4.5 > 100
*

All compounds had a CC50 of > 1 μM in Huh-7 cells