Table 1.
Anti-HIV Activity and Cytotoxicity in MT-4 Cells Infected with HIV-1 IIIB and HIV-2 ROD.
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Compound ID | R1 | R2 | EC50 a (μM) | CC50 b (μM) | SI c | ||
HIV-1 IIIB | HIV-2 ROD | HIV-1 | HIV-2 | ||||
FTC-2 | F | H | 5.36 ± 0.98 | 15.56 ± 1.06 | >265.69 | >49.57 | >17.08 |
TC-2 | H | H | 29.07 ± 4.23 | 19.72 ± 6.42 | 261.13 ± 33.14 | 8.98 | 13.24 |
TD-1a | H |
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16.81 ± 0.91 | 4.86 ± 1.71 | 86.54 ± 29.24 | 5.15 | 17.81 |
TD-1b | H |
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>34.80 | 16.22 ± 17.16 | 34.80 ± 5.75 | N.D.d | 2.15 |
TD-1c | H |
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18.90 ± 2.66 | 6.59 ± 1.63 | 61.65 ± 8.44 | 3.26 | 9.36 |
TD-1d | H |
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17.88 ± 2.68 | 7.92 ± 0.83 | 81.42 ± 22.66 | 4.55 | 10.28 |
TD-1e | H |
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>25.48 | >25.48 | 25.48 ± 2.90 | N.D. | N.D. |
TD-1f | H |
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>23.51 | >23.51 | 23.51 ± 2.79 | N.D. | N.D. |
TD-1g | H |
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25.60 ± 7.51 | 20.48 ± 8.49 | 58.27 ± 4.85 | 2.28 | 2.85 |
TD-1h | H |
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29.62 ± 4.34 | 10.67 ± 3.66 | 53.13 ± 5.12 | 1.79 | 4.98 |
TD-1i | H |
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19.09 ± 5.08 | 15.25 ± 0.55 | 96.17 ± 19.83 | 5.04 | 6.31 |
TD-1j | H |
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16.77 ± 0.78 | 17.83 ± 2.79 | 137.19 ± 22.50 | 8.18 | 7.69 |
TD-1k | H |
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>27.59 | >27.59 | 27.59 ± 3.18 | N.D. | N.D. |
TD-1l | H |
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>31.87 | >31.87 | 31.87 ± 1.73 | N.D. | N.D. |
TD-1m | H |
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>189.23 | 17.14 ± 2.49 | 189.23 ± 2.19 | N.D. | 11.04 |
PF74 | - | - | 1.08 ± 0.24 | 5.76 ± 2.14 | >293.75 | >271.99 | >51.00 |
a EC50: the concentration of the compound required to achieve 50% protection of MT-4 cells against the HIV-induced cytotoxicity effect, determined in at least triplicate against HIV in MT-4 cells; b CC50: the concentration of the compound required to reduce the viability of uninfected cells by 50%, determined in at least triplicate against HIV in MT-4 cells; values were averaged from at least three independent experiments; c SI: selectivity index, the ratio of CC50/EC50. d N.D.: not determined.