Table 1.
Efficacy and microsomal stability of the active AR-NTD inhibitors.

| VPCID | R1 | R2 | R4 | R5 | R6 | R8 | eGFP IC50 (μM) | PSA IC50 (μM) | PC3-iV7 IC50 (μM) | T1/2 (min.) |
|---|---|---|---|---|---|---|---|---|---|---|
| 220009 |
|
|
1 | 1 | NA | |||||
| 220010 |
|
|
0.5 | 0.7 | 2.3 | 30 | ||||
| 220027 |
|
Br |
|
Br | 3 | 4 | 4 | TBD | ||
| 220028 |
|
Br |
|
Br | 0.4 | 0.4 | 3 | NA | ||
| 220054 |
|
|
|
5 | 5 | 3 | NA | |||
| 220057 |
|
|
|
|
10 | 8 | 8 | 462 | ||
| 220062 |
|
Br |
|
0.5 | 0.5 | 3 | 36 | |||
| 220075 |
|
|
0.5 | 0.5 | 12 | 18 | ||||
| RR-220010 |
|
|
0.7 | 0.7 | 5 | 11 | ||||
| SS-220010 |
|
|
0.7 | 0.6 | 6 | 12 | ||||
| RS-220010 |
|
|
0.85 | 0.79 | 5 | 15 |