Table 1. RNase H Inhibition of the Newly Synthesized Compounds 6a–h, 7a–h, 8a–c, 9a–c, 10a–i, and 11a–i.
cpd | IC50 (μM)a | cpd | IC50 (μM)a | cpd | IC50 (μM)a |
---|---|---|---|---|---|
6a | 14.3 ± 2.35 | 7g | 63 ± 7.0 | 10g | 6.8 ± 0.4 |
6b | >100 | 7h | 13.7 ± 1.3 | 10h | 7.9 ± 0.7 |
6c | >100 | 8a | >100 | 10i | 25.8 ± 3.7 |
6d | >100 | 8b | >100 | 11a | 3.21 ± 0.94 |
6e | >100 | 8c | >100 | 11b | 0.27 ± 0.05 |
6f | 9.4 ± 0.2 | 9a | >100 | 11c | 2.38 ± 0.59 |
6g | 97 ± 5.0 | 9b | >100 | 11d | 4.50 ± 0.60 |
6h | 9.4 ± 0.7 | 9c | >100 | 11e | 1.73 ± 0.31 |
7a | 75 ± 4.5 | 10a | 5.4 ± 1.2 | 11f | 70 ± 8 |
7b | >100 | 10b | 17.8 ± 1.2 | 11g | 23 ± 3 |
7c | >100 | 10c | 8.5 ± 1.6 | 11h | 5.8 ± 1.4 |
7d | >100 | 10d | 5.50 ± 0.93 | 11i | 9.2 ± 0.4 |
7e | >100 | 10e | 4.15 ± 0.55 | 1 | 10 ± 1.2 |
7f | 25.3 ± 5.3 | 10f | 8.1 ± 0.4 |
Inhibitory concentration 50% (μM) determined from dose–response curves: experiments performed against HIV-1 RT-associated RNase H activity.
Bn, benzyl.