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. 2018 Aug 8;9(9):941–946. doi: 10.1021/acsmedchemlett.8b00296

Table 1. SAR of the Aniline Ringa.

graphic file with name ml-2018-00296t_0005.jpg

Compd R′ EC50 (μM)b Rel. Act. (%)c
1 3′-Cl 9.7 ± 1.16 96 ± 13.9
2 H 47 ± 13.6
3 3′-Me 16.4 ± 0.35 96 ± 2.1
4 3′-Br 7.1 ± 1.93 87 ± 12.5
5 3′-OMe 38 ± 8.5
6 3′-(1-hydroxyethyl) 10 ± 4.8
7 4′-Me 8 ± 1.4
8 4′-Br 16 ± 4.0
9 4′-OMe 19 ± 0.9
10 3′,4′-diMe 37 ± 11.3
11 3′,5′-diMe 44 ± 20.4
12 3′,4′-diCl 22 ± 5.6
13 3′,5′-diCl 41 ± 26.5
14 3′-Cl-4′-F 13.1 ± 1.20 96 ± 10.6
a

Each value represents the mean ± SD of at least two separate experiments.

b

“—” denotes an EC50 value of >100 μM or an EC50 value that was not calculated due to low efficacy in vitro.

c

Activation values represent the percentage activation for each compound relative to the activation of a positive control compound.14,16,17