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