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. 2020 Mar 5;11(5):798–805. doi: 10.1021/acsmedchemlett.9b00617

Table 1. RNase H Inhibition of the Newly Synthesized Compounds 6ah, 7ah, 8ac, 9ac, 10ai, and 11ai.

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    
a

Inhibitory concentration 50% (μM) determined from dose–response curves: experiments performed against HIV-1 RT-associated RNase H activity.

b

Bn, benzyl.