3-Phenylcoumarins as Inhibitors of HIV-1 Replication
Abstract
:1. Introduction
2. Results and Discussion
Compound | Antiviral activity | ||||||
---|---|---|---|---|---|---|---|
5.1 + TNFα | Hela-Tat-luc | HeLa-Tet-ON | RV (VIH) | Toxicity (%) | |||
25 µM | 50 µM | 25 µM | 50 µM | 50 µM | IC50, µM | CC50 | |
7 | nt | 21.7 ± 3 | 26.8 ± 2.9 | 33.7 ± 1.0 | S | 130 ± 11.4 | >50 |
8 | nt | −28.7 ± 4 | nt | 17.6 ± 2.1 | S | 20.7 ± 1.9 | >50 |
9 | nt | 33.0 ± 2.33 | nt | −4.9 ± 0.8 | nt | >195 | >50 |
10 | nt | 61.2 ± 2.4 | 73.5 ± 6.7 | 66.6 ± 3.4 | U | 73 ± 8.6 | >50 |
11 | 84.3 ± 3 | 81.6 ± 5.6 | 77.5 ± 8.5 | 80.1 ± 5.6 | U | 18.2 ± 0.2 | >50 |
12 | nt | −40.9 ± 2.3 | nt | 14.1 ± 0.6 | S | >172 | >50 |
13 | nt | 68.5 ± 3.4 | 32.8 ± 4.3 | 39.5 ± 2.3 | S | 138 ± 22,3 | 16.7 ± 3.4 |
14 | nt | −23.0 ± 2.9 | nt | −25.1 ± 5.3 | nt | >177 | >50 |
15 | nt | 49.7 ± 7.0 | 47.6 ± 6.2 | 35.1 ± 3.9 | U | 62.7 ± 13.1 | 42.8 ± 16.2 |
16 | nt | 59.0 ± 8.2 | nt | 17.2 ± 0.5 | S | 81.4 ± 14.0 | >50 |
17 | 82.2 ± 3.1 | 87.8 ± 9.8 | 85.7 ± 3.4 | 88.3 ± 5.5 | U | 84.6 ± 12.1 | >50 |
18 | nt | −3.5 ± 0.9 | nt | 22.8 ± 3.4 | S | 186 ± 10.8 | >50 |
19 | −34.26 ± 5 | −4.7 ± 0.3 | 48.9 ± 3.4 | 55.7 ± 4.9 | S | 23.8 ± 1.7 | >50 |
20 | nt | −21.2 ± 7.0 | nt | −64.4 ± 10 | nt | >209 | 18.4 ± 8.2 |
Mesuol | 71.0 ± 4.8 | 77.9 ± 4.9 | nt | 71.3 ± 8.9 | S | 2.5 | >4 µM |
AZT | nt | nt | nt | nt | nt | 0.01 | >1 µM |
3. Experimental
3.1. Material and Reagents
3.2. General Procedure for the Synthesis of Compounds 7–20
3.3. Anti-HIV Bioassay
4. Conclusions
Acknowledgments
References
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Olmedo, D.; Sancho, R.; Bedoya, L.M.; López-Pérez, J.L.; Del Olmo, E.; Muñoz, E.; Alcamí, J.; Gupta, M.P.; San Feliciano, A. 3-Phenylcoumarins as Inhibitors of HIV-1 Replication. Molecules 2012, 17, 9245-9257. https://doi.org/10.3390/molecules17089245
Olmedo D, Sancho R, Bedoya LM, López-Pérez JL, Del Olmo E, Muñoz E, Alcamí J, Gupta MP, San Feliciano A. 3-Phenylcoumarins as Inhibitors of HIV-1 Replication. Molecules. 2012; 17(8):9245-9257. https://doi.org/10.3390/molecules17089245
Chicago/Turabian StyleOlmedo, Dionisio, Rocío Sancho, Luis M. Bedoya, José L. López-Pérez, Esther Del Olmo, Eduardo Muñoz, José Alcamí, Mahabir P. Gupta, and Arturo San Feliciano. 2012. "3-Phenylcoumarins as Inhibitors of HIV-1 Replication" Molecules 17, no. 8: 9245-9257. https://doi.org/10.3390/molecules17089245