Table 9.
Heterocycle Analogues: Anti-HIV-1 Activity (EC50) and Cytotoxicity (CC50)
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|---|---|---|---|---|---|---|---|
| compd | R | R′ | R″ | W | Y | EC50a(µM) | CC50a(µM) |
| 21 | Cl | Cl | H | S | N | NA | >100 |
| 22 | Cl | Cl | H | S | CH | 3.1 | 29 |
| 23 | Cl | Cl | Cl | S | CH | 1.4 | 9.8 |
| 24 | Cl | CN | H | S | CH | 0.43 | >100 |
| 25 | Cl | Et | H | O | CH | 2.8 | >100 |
| 26 | Cl | F | H | O | CH | 0.43 | 12 |
| 27 | Cl | Cl | H | O | CH | 0.11 | 2.8 |
| 28 | Cl | CN | H | O | CH | 0.022 | 2.1 |
| 29 | F | CN | H | O | CH | 0.013 | 7.4 |
See footnotes in Table 4. NA for EC50> CC50.
