Table 1.
No. | Name | Formula | R1 a | R2 a | CD40 IC50 [μM] | OX40 IC50 [μM] | BAFF IC50 [μM] | TNF IC50 [μM] | NF-κB IC50 [μM] |
---|---|---|---|---|---|---|---|---|---|
6 | DRI-C21041 | C30H21N3O7S | 1-SO3H | 4′-NO2 | 0.087 | 317.9 | 0.328 | >1000 | 19.9 |
7 | DRI-C24041 | C30H21N3O7S | 4-SO3H | 4′-NO2 | 0.299 | 9.34 | 2.007 | 554.6 | |
8 | DRI-21047a | C31H21F3N2O5S | 1-SO3H | 4′-CF3 | 57.85 | 10.07 | 42.18 | 61.07 | |
9 | DRI-C24541 | C32H23N3O6 | 4-CO2Me | 4′-NO2 | 55.99 | >1000 | 685.6 | 795.8 | |
10 | DRI-C2105041 | C30H21N3O10S2 | 1,5-(SO3H)2 | 4′-NO2 | 68.31 | 135.0 | 439.7 | 688.5 | |
11 | DRI-C2105045 | C32H24N2O10S2 | 1,5-(SO3H)2 | 4′-CO2Me | 60.07 | 120.4 | 540.1 | 456.1 | |
12 | DRI-C2104121 | C30H20N4O9S | 1-SO3H | 2′,4′-(NO2)2 | 50.50 | 10.31 | 38.14 | 61.68 | |
13 | DRI-C2104531 | C32H23N3O9S | 1-SO3H | 3′-NO2-4′-CO2Me | 0.390 | 86.19 | 5.27 | 674.4 | |
14 | DRI-C21091 | C36H25N3O7S | 1-SO3H | 4′-(4-NO2)C6H4 | 0.020 | 6.88 | 0.784 | 70.35 | 11.1 |
15 | DRI-C21095 | C38H28N2O7S | 1-SO3H | 4′-(4-CO2Me)C6H4 | 0.019 | 1.013 | 1.517 | 26.55 | 6.0 |
16 | DRI-C31041 | C32H25N3O7S | 1-SO3H | 4′-NO2 | 44.80 | 7.28 | 26.73 | 61.48 | |
17 | DRI-C41041 | C28H19N3O7S | 1-SO3H | 4′-NO2 | 57.45 | 36.63 | 81.38 | 118.5 | |
18 | DRI-C61041 | C29H20N4O7S | 1-SO3H | 4′-NO2 | 1.34 | 5.48 | 8.07 | 46.94 | 8.7 |
19 | DRI-C61045 | C31H23N3O7S | 1-SO3H | 4′-CO2Me | 2.41 | 6.97 | 13.76 | 182.0 |
a For numbering, see structure 6 in Scheme 1.