Fluorine Substituted 1,2,4-Triazinones as Potential Anti-HIV-1 and CDK2 Inhibitors
Table 1
Anti-HIV-1 activities of fluorinated 1,2,4-triazinones 1–18.
Compounds
EC50 (μM)a
CC50 (μM)b
SIc
1
10.8 ± 1.0
25 ± 1.0
2.51
0.64
3
20 ± 1.0
49 ± 1.0
2.50
2.09
5
25 ± 1.0
75 ± 1.0
3.00
2.4
6
30 ± 1.0
60 ± 1.0
2.00
2.39
9
35 ± 1.0
75 ± 1.0
2.20
4.41
10
42 ± 1.0
82 ± 1.0
2.11
3.04
11
6.6 ± 1.0
44 ± 2.0
7.15
4.44
14
5.8 ± 1.0
35 ± 1.0
6.2
3.56
15
14.0 ± 1.0
29 ± 1.0
2.01
2.67
16
6.9 ± 1.0
36 ± 1.1
5.1
7.07
17
25 ± 1.8
76 ± 1.0
3.01
—
18
50 ± 1.1
90 ± 2.1
1.8
3.69
EC50: inhibiting p24 production in the MT-4 cells. CC50: concentration of compound that reduces the viability of mock-infected cells by 50%, as determined by the MTT method. SI: selectivity index; CC50/EC50.
