Table 6.
Pro-drug SAR studies: Examples of ester pro-drugs [56].
| Prodrug Derivatives of Integrase Inhibitors | Prodrug Anti-HIV EC50 (MAGI Cell) * | Diketo Acid Anti-HIV EC50 (MAGI Cell) * |
|---|---|---|
101 |
300 nM | 2100 nM (Compound 41) |
102 |
>5000 nM | 710 nM (Compound 98) |
103 |
>5000 nM | 710 nM (Compound 98) |
104 |
1900 nM | 710 nM (Compound 98) |
105 |
5300 nM | 710 nM (Compound 98) |
106 |
1600 nM | 710 nM (Compound 98) |
107 |
40 nM | 700 nM (Compound 55) |
108 |
3900 nM | 700 nM (Compound 55) |
109 |
50 nM | 300nM (Compound 51) |
110 |
>5000 nM | 700 nM (Compound 71) |
111 |
15 nM | 600 nM (Compound91) |
112 |
400 nM | 420 nM (Compound 99) |
113 |
100 nM | 1300 nM (Compound 94) |
114 |
110 nM | 1300 nM (Compound 97) |
115 |
226 nM | 1000 nM (Compound 95) |
116 |
9 nM | 500 nM (Compound 96) |
117 |
176 nM | 800 nM (Compound 64) |
118 |
1200 nM | 500 nM (Compound 100) |
119 |
400 nM | 600 nM (Compound 69) |
120 |
4400 nM | 1400 nM (Compound 73) |
121 |
2700 nM | 700 nM (Compound 71) |
* EC50 = concentration for 50% inhibition of the replication of HIV-1.