Table 1.
Compound | Binding to cyclophilinA, KD (M) |
IC50 for inhibition of PPIase activity (µM) |
% Inhibition of HIV-1 replication |
CC50 (µM) |
---|---|---|---|---|
FD1 | 7.67±0.12×10−5 | 70.2±3.04 | 26.7 | >100 |
FD2 | 6.78±0.08×10−5 | 72.8±1.12 | 23.0 | >100 |
FD3 | 7.33±0.26×10−5 | 65.7±2.55 | 29.9 | >100 |
FD4 | 2.11±0.15×10−5 | 56.2±0.97 | 22.5 | >100 |
FD5 | 6.61±0.09×10−6 | 14.45±0.67 | 57.2 | 14.46±0.59 |
FD6 | 9.19±1.03×10−6 | 21.65±2.20 | 18.2 | 41.81±2.52 |
FD7 | 3.61±0.25×10−5 | 43.75±1.15 | 33.7 | 73.75±0.67 |
FD8 | 8.42±0.13×10−6 | 18.67±1.74 | 62.6 | 40.91±0.59 |
FD9 | 1.03±0.16×10−5 | 34.86±0.76 | 77.5 | 54.24±4.96 |
FD10 | 5.95±0.24×10−6 | 6.98±1.39 | 64.2 | 65.66±4.77 |
FD11 | 4.72±0.27×10−5 | 53.4±1.63 | 44.9 | 71.46±4.13 |
FD12 | 3.19±0.22×10−6 | 3.47±0.92 | 65.2 | 69.73±0.75 |
Cyclosporin A | 2.18±0.36×10−7 | 0.45±0.38 | 98.9 | 6.26±0.28 |