Table 3.
In vitro growth inhibitory effects of compounds with protection on B ring
| Structure | ID | R1 | R2 | IC50 ± SEM (nM) |
||||||
|---|---|---|---|---|---|---|---|---|---|---|
| A375 | B16-F1 | WM164 | LNCaP | PC-3 | Du 145 | PPC-1 | ||||
 |
4ab | H | 4-OMe | >10000 | >10000 | >10000 | >10000 | >10000 | >10000 | >10000 |
| 4ac | H | 3-OMe | >10000 | >10000 | >10000 | >10000 | >10000 | >10000 | >10000 | |
| 4ah | H | 4-Me | >10000 | >10000 | >10000 | >10000 | >10000 | >10000 | >10000 | |
| 4af | H | 4-F | 630±72 | 946±86 | 596±61 | 573 | 2233 | 846 | 575 | |
| 4ag | H | 3-F | >10000 | >10000 | >10000 | >10000 | >10000 | >10000 | >10000 | |
| 4cb | 4-OMe | 4-F | 36±5 | 71±8 | 43±6 | 31±2 | 33±2 | 52±3 | 32±0.7 | |
| 4db | 4-Me | 4-F | 113±14 | 287±31 | 107±14 | 55±3 | 80±1 | 80±1 | 57±1 | |
| 4ea | 3,4,5-(OMe)3 | 3,4,5-(OMe)3 | >10000 | >10000 | >10000 | >10000 | >10000 | >10000 | >10000 | |
| 4eb | 3,4,5-(OMe)3 | 4-F | 3840 | >10000 | >10000 | >10000 | >10000 | >10000 | >10000 | |
| 4fb | 4-Cl | 4-F | 88±9 | 107±12 | 70±6 | 48±1 | 76±2 | 64±1 | 54±1 | |
| 4ga | 4-N(Me)2 | 3,4,5-(OMe)3 | 162±13 | 1200±90 | 308±32 | 62±2 | 93±6 | 99±2 | 72±0.4 | |
| 4gb | 4-N(Me)2 | 4-F | 55±7 | 242±26 | 56±4 | 56±6 | 83±3 | 74±0.5 | 48±0.3 | |
| 4ha | 3,4-(OMe)2 | 3,4,5-(OMe)3 | 192±15 | 970±68 | 139±15 | 114±6 | 197±9 | 144±29 | 117±2 | |
| 4hb | 3,4-(OMe)2 | 4-F | 960±59 | 2000±400 | 1400±30 | 1915±77 | 10000 | 3312 | 1441±49 | |
| 4ia | 2-CF3 | 3,4,5-(OMe)3 | >10000 | >10000 | >10000 | >10000 | >10000 | >10000 | >10000 | |
| 4ib | 2-CF3 | 4-F | >10000 | >10000 | >10000 | >10000 | >10000 | >10000 | >10000 | |
| 4jb | 4-OBn | 4-F | 64±7 | 110±15 | 48±5 | 35±1 | 75±0.5 | 58±1 | 38±0.2 | |