TABLE 1.
Inhibition potencies of IAS derivatives against HIV-1 wild-type RT and NNRTI-resistant mutants
| Compound | ID50 (nM) fora
|
||||||
|---|---|---|---|---|---|---|---|
| wt | Leu100Ile | Lys103Asn | Val106Ala | Val179Asp | Tyr181Ile | Tyr188Leu | |
| RS1202 | 1 (±0.1) | 100 (±20) | 5 (±1) | 75 (±8) | 35 (±3) | 140 (±10) | 1,000 (±100) |
| RS1588 | 3 (±0.1) | 60 (±6) | 3 (±0.5) | 90 (±8) | 50 (±5) | 140 (±10) | 200 (±20) |
| RS1866 | 2.2 (±0.1) | n.d. | 750 (±60) | n.d. | n.d. | 1,500 (±100) | n.d. |
| RS1980 | 3 (±0.2) | n.d. | 500 (±50) | n.d. | n.d. | 130 (±10) | n.d. |
| Nevirapine | 400 (±50) | 900 (±90) | 2,000 (±80) | 2,000 (±300) | 300 (±25) | 5,000 (±400) | 5,000 (±400) |
| Efavirenz | 40 (±0.5) | n.d. | 1,000 (±40) | n.d. | n.d. | 400 (±50) | n.d. |
a
ID50, concentration of the inhibitor that reduced the in vitro activity of HIV-1 RT by 50% under the conditions described in Materials and Methods. Numbers are the mean values of three independent experiments (standard deviations are in brackets). wt, wild type; n.d., not determined.