Table 1.
Summary of binding data for compounds of the present study.
| No. | Formula | Linker | R1a | R2a | CD40 IC50 [µM] |
TNF IC50 [µM] |
NF-κB IC50 [µM] |
B cell IC50 [µM] |
|---|---|---|---|---|---|---|---|---|
| 1 | C45H32N10O21S6 | 2.26 | 42.7 | |||||
| 5 | C24H17N3O7S | benzene | 1-SO3H | 4’-NO2 | 341.6 | >1000 | ||
| 6 | C30H21N3O7S | biphenyl | 1-SO3H | 4’-NO2 | 0.31 | >1000 | 10.3 | 13.2 |
| 7 | C30H21N3O7S | biphenyl | 5-SO3H | 4’-NO2 | 2.33 | 478.6 | ||
| 8 | C30H23N3O5S | biphenyl | 1-SO3H | 4’-NH2 | 301.0 | 886.9 | ||
| 9 | C30H21N5O5S | biphenyl | 1-SO3H | 3’,4’-(N=N-NH)- | 0.99 | >1000 | ||
| 10 | C32H24N2O7S | biphenyl | 1-SO3H | 4’-CO2Me | 0.17 | 992.0 | 17.1 | 4.5 |
| 11 | C31H21N3O6 | biphenyl | 5-CO2H | 4’-NO2 | 0.36 | >1000 | 9.4 | 15.9 |
a
For numbering, see structure 6 in Scheme 1.