TABLE 5.
Cross-resistance phenotype of calanolide-resistant viruses
| Compound | EC50 (μM) for viruses with following phenotypes (resistance mutation)a
|
|||
|---|---|---|---|---|
| Calanolide A resistant (T139I) | Costatolide resistant (L100I, T139I) | Dihydrocostatolide resistant (L100I) | Wild type (strain IIIB) | |
| Calanolide A | >27 | >27 | 7.2 | 0.1 |
| Costatolide | 4.5 | >27 | >27 | 0.1 |
| Dihydrocostatolide | >27 | >27 | >27 | 0.2 |
| UC10 | 0.3 | 2.6 | 1.0 | 0.1 |
| NSC 676509 | 0.4 | >2 | 1.0 | 0.05 |
| UC781 | 0.04 | 0.04 | 0.3 | 0.005 |
| NSC 675187 | 0.03 | 0.08 | 0.03 | 0.05 |
| Thiazolobenzimidazole | 3.9 | >69 | 22.8 | 2.5 |
| Oxathiin carboxanilide | 1.6 | >28 | >28 | 0.5 |
| TIBO | 0.4 | >35 | 11.7 | 0.1 |
| Diphenylsulfone | 16.0 | 85 | 53.1 | 3.7 |
| TSAO | 0.5 | 0.3 | 0.05 | 0.05 |
| α-APA | 0.07 | 0.09 | 0.02 | 0.03 |
| E-BPTU | 0.01 | 3.0 | 0.08 | 0.04 |
| Nevirapine | 0.03 | 0.2 | 0.1 | 0.01 |
| AZT | 0.01 | 0.06 | 0.003 | 0.005 |
| 3TC | 0.1 | 0.04 | 0.03 | 0.07 |
a
EC50s are the means for a minimum of two replicate evaluations. The reproducibilities of the EC50s obtained between replicate experiments in this highly optimized anti-HIV assay have been determined to be such that the standard errors averaged less than 10% of the respective mean value.