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. 2012 Dec 2;4(1):113–117. doi: 10.1021/ml300335r

Table 1. Preliminary SAR around Compound 6: Methyl-Walk, Antiviral, and FASN Inhibitory Activities.

graphic file with name ml-2012-00335r_0004.jpg

compd R1 R2 R3 R4 hFASNa (IC50, μM) rFASNb (IC50, μM) HCVc (EC50, μM) CC50d (IC50, μM) SIe
6 Me H H H 0.107 1.72 0.175 >20 >114
7 H H H H 0.130 2.95 0.550 >3.0 >5.0
8 H Me H H >50 >50 >10 >10 N/A
9 H H Me H 0.060 0.635 0.150 8.6 57
10 H H H Me >50 >50 >10 1.9 <0.19
a

Biochemical inhibition of human FASN.

b

Biochemical inhibition of rat FASN.

c

Inhibition of HCV RNA in the replicon system. Telaprevir was used as a positive control.

d

Inhibition of cell viability.

e

SI = EC50/CC50; n ≥ 2, and CV ≤ 50%.