Table 7.
Benzylic Analogues: Anti-HIV-1 Activity (EC50) and Cytotoxicity (CC50)
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|---|---|---|---|---|---|---|
| compd | R | R′ | X | Y | EC50a(µM) | CC50a(µM) |
| 8 | Cl | Cl | CH2 | NH | 0.82 | 20 |
| 15 | Cl | Cl | NH | NH | > 100 | > 100 |
| 16 | Cl | Cl | CH2 | CH2 | 18 | 43 |
| 13 | Cl | CN | CH2 | NH | 0.13 | 40 |
| 17 | Cl | CN | NH | NH | 9.8 | > 100 |
| 18 | Cl | CN | NCH3 | NH | 0.27 | > 100 |
| 19b | Cl | CN | CHCH3 | NH | 1.20 | 54 |
| 20b | F | CN | CHCH3 | NH | 0.13 | 8.5 |
See footnotes in Table 4.
Racemate.
