Table 5.
Anti-HIV Activity (EC50) and Average Cytotoxicity (CC50), μM, of Catechol Diether Derivatives and Reference NNRTIs for WT and Viral Variants.
Compd | EC50 |
CC50 | ||
---|---|---|---|---|
WT | Y181C | K103N/Y181C | ||
20 | 0.14 | 21 | 2.2 | 77 |
22 | 0.090 | 6.7 | 1.2 | 32 |
25 | 0.014 | 0.52 | 1.7 | >100 |
26 | 0.013 | 0.62 | 1.7 | 13 |
27 | 0.017 | 0.24 | 0.57 | 21 |
31 | 0.043 | 0.92 | 2.8 | 59 |
32 | 0.020 | 0.80 | >43 | >61 |
40 | 0.015 | 0.98 | 8.0 | >90 |
41 | 0.005 | 0.37 | 1.6 | 22 |
42 | 0.000055 | 0.049 | 0.22 | 10 |
43 | 0.0032 | 0.15 | 0.90 | 48 |
44 | 0.00032 | 0.016 | 0.085 | 45 |
45 | 0.020 | 2.8 | ND | 30 |
nevirapine | 0.11 | >100 | >100 | >100 |
nevirapinea | 0.081 | >10 | >10 | |
efavirenz | 0.002 | 0.010 | 0.030 | 15 |
efavirenza | 0.0014 | 0.002 | 0.037 | |
etravirine | 0.001 | 0.008 | 0.005 | 11 |
etravirinea | 0.001 | 0.007 | 0.004 | |
rilpivirine | 0.00067 | 0.00065 | 0.002 | >1 |
rilpivirinea | 0.0004 | 0.0013 | 0.001 | 8 |
Literature data; see ref. 28.