Table 2.
A synopsis of the SARs associated with indole substitution patterns in HIV-1 AIs
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---|---|---|---|---|---|---|
Compd | R1 | R2 | R3 | R4 | EC50 (nM) | CC50 (μM) |
15 | F | H | H | H | 2.6 | >300 |
27 | Cl | H | H | H | 4.3 | 212 |
28 | CH3O | H | H | H | 0.52 | >300 |
29 | CH3CH2O | H | H | H | 0.45 | >95 |
30 | iPrO | H | H | H | >500 | 150 |
31 | H | F | H | H | 838.3 | >300 |
32 | H | Cl | H | H | 395 | 46 |
33 | H | CH3O | H | H | 21,100 | >300 |
34 | H | H | F | H | 21.1 | >245 |
35 | H | H | Cl | H | 208 | >110 |
36 | H | H | CH3O | H | 328.8 | >300 |
37 | H | H | H | F | 7.3 | >152 |
38 | H | H | H | Cl | 4.4 | 162 |
39 | H | H | H | CH3O | 6.6 | 153 |
40 | F | H | H | F | 0.35 | >300 |
41 | F | H | H | CH3O | 0.06 | >300 |
42 | CH3O | H | H | CH3O | 0.23 | 279 |
43 | CH3O | H | H | Cl | 0.07 | >300 |