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. 2010 Apr 6;1(4):165–169. doi: 10.1021/ml100013s

Table 2. SAR of S-Linked Seriesa.

  X IC50 L929   X IC50 L929
thioether
5 2-Cl 0.58 >10 21 2-CO2Me 0.14 >10
6 3-Cl 0.12 1.11 22 3-OMe 0.12 2.64
7 4-Cl 0.15 2.02 23 4-NHCOMe 0.04 >10
8 3,4-Cl2 0.49 0.56 24 4-NH2 0.03 >10
20 4-NO2 0.32 >10        
sulfoxide
10 2-Cl 0.18 >10 12 4-Cl 0.12 8.87
11 3-Cl 0.15 >10 13 3,4-Cl2 0.30 2.67
sulfone
15 2-Cl 0.10 >10 17 4-Cl 0.16 >10
16 3-Cl 0.22 >10 18 3,4-Cl2 0.52 >10
a

IC50: growth inhibition of T. b. brucei 427 strain (μg/mL). L929: IC50 against L929 cells (μg/mL). References: suramin and pentamidine.