TABLE 1.
Structure and antiviral activity of INSTIs in the MT-2 cell line
INSTIa | Structure | Antiviral activity against HIV-1, EC50 (nM)b (fold change) |
|
---|---|---|---|
WT | G140S+Q148H | ||
BIC | ![]() |
1.5 ± 0.2 | 3.1 ± 0.8 (2.1) |
DTG | ![]() |
1.5 ± 0.2 | 6.5 ± 1.2 (4.3) |
RAL | ![]() |
9.4 ± 1.4 | 2,461 ± 323 (262) |
EVG | ![]() |
2.1 ± 0.9 | 868 ± 138 (413) |
Compound 1 | ![]() |
1.4 ± 0.5 | 4.5 ± 1.8 (3.2) |
Compound 2 | ![]() |
1.5 ± 0.5 | 11.1 ± 0.5 (7.4) |
All compounds were synthesized at Gilead Sciences, Inc.
EC50, 50% effective concentration.