TABLE 2.
Antiviral and immunosuppressive activity and TI values of compounds after a 2-week treatment of MO-DC/CD4+-T-cell cocultures
| Compound | Geometric mean (range)d
|
TIc | |
|---|---|---|---|
| EC50 (nM)a | ISC50 (nM)b | ||
| PMPA | 89 (58-200) | >100,000 | >1,124 |
| UC-781 | 50 (30-84) | 28,921 (8,973-71,010) | 578 |
| R165335 | 3 (2-4) | 21,735 (21,021-22,473) | 7,245 |
| R147681 | 2 (0.44-5) | 1,633 (1,000-3,093) | 816 |
| R152929 | 1 (0.41-2.3) | 2,781 (2,261-3,531) | 2,781 |
| R153430 | 0.74 (0.26-3) | 2,372 (1,662-3,217) | 3,205 |
| R152649 | 0.47 (0.29-0.6) | 3,651 (1,691-7,083) | 7,768 |
| R278474 | 0.42 (0.32-0.55) | 1,216 (622-2,908) | 2,895 |
| R151694 | 0.40 (0.039-3) | 158 (76-440) | 395 |
| R302730 | 0.24 (0.05-0.55) | 43,208 (36,023-51,825) | 180,033 |
| R312924 | 0.05 (0.004-0.051) | 20,240 (15,650-26,924) | 404,800 |
a
That is, the concentration of compound required to inhibit 50% of HIV-1 Ba-L replication after a 2-week treatment of cocultures of HIV- infected MO-DC and CD4+ T cells.
b
That is, the, concentration of compound required to inhibit 50% of the T-lymphocyte proliferation, as measured in mixed leucocyte cultures of MO-DC and allogeneic CD4+ T cells.
c
That is, the ISC50/EC50 ratio.
d
All compounds were evaluated in sixfold replicates in at least three different experiments.