Table 2.
Anti-Proliferative Activity of Diheteroarylnona-1,3,6,8-tetraen-5-ones
| Compd. | IC50 (μM)a | IC50 (curcumin)/IC50(dienone) | ||||
|---|---|---|---|---|---|---|
| PC-3b | DU145c | LNCaPd | PC-3b | DU145c | LNCaPd | |
| Curcumin | 25.43 ± 2.15 | 26.23 ± 0.65 | 13.61 ± 2.69 | 1 | 1 | 1 |
| 59 | 6.21 ± 0.15 | 6.38 ± 0.65 | 6.85 ± 0.35 | 4 | 4 | 2 |
| 60 | 3.00 ± 1.18 | 7.37 ± 1.44 | 8.01 ± 2.87 | 9 | 4 | 2 |
| 61 | 10.47 ± 2.43 | 5.30 ± 2.36 | 8.09 ± 1.20 | 2 | 5 | 2 |
| 62 | 4.19 ± 0.24 | 4.19 ± 1.35 | 2.58 ± 1.04 | 6 | 6 | 5 |
| 63 | 24.77 ± 8.06 | 11.35 ± 2.96 | >20 | 1 | 2 | <1 |
| 64 | >20 | 18.53 ± 10.59 | >20 | <1 | 1 | <1 |
| 65 | 3.86 ± 0.23 | 2.45 ± 1.29 | 6.14 ± 2.68 | 7 | 11 | 5 |
| 66 | 7.43 ± 4.05 | 2.69 ± 0.99 | 4.94 ± 0.47 | 3 | 10 | 5 |
| 67 | >15 | >15 | > 20 | <1.7 | <1.7 | <1 |
| 68 | 2.36 ± 0.56 | 1.21 ± 0.43 | 2.43 ± 1.31 | 11 | 22 | 6 |
| 69 | 2.50 ± 1.06 | 1.75 ± 0.52 | 5.62 ± 3.57 | 10 | 15 | 2 |
| 70 | 45.69 ± 19.56 | 3.59 ± 2.63 | 17.53 ± 4.89 | <1 | 7 | <1 |
| 71 | 10.39 ± 4.71 | 8.29 ± 2.97 | 6.05 ± 4.93 | 3 | 3 | 2 |
| 72 | 5.22 ± 3.97 | 6.55 ± 3.26 | 4.94 ± 0.47 | 5 | 4 | 3 |
| 73 | >15 | >15 | 5.89 ± 2.64 | <1.7 | <1.7 | 2.3 |
| 74 | 1.79 ± 0.24 | 1.60 ± 0.08 | 1.63 ± 0.34 | 14 | 16 | 8 |
| 75 | 1.14 ± 0.12 | 1.78 ± 0.13 | 2.17 ± 0.2 | 22 | 15 | 6 |
| 76 | 11.74 ± 0.61 | 14.36 ± 0.34 | 13.62 ± 3.64 | 2 | 2 | 1 |
| 77 | >15 | >15 | 17.71 ± 4.88 | <1.7 | <1.7 | <1 |
| 78 | 1.09 ± 0.17 | 1.20 ± 0.01 | 0.98 ± 0.19 | 23 | 22 | 14 |
| 79 | 2.63 ± 0.51 | 3.50 ± 0.17 | 0.97 ± 0.34 | 10 | 8 | 14 |
| 80 | 2.48 ± 0.41 | 2.70 ± 0.28 | 1.49 ± 2.24 | 10 | 10 | 9 |
| 81 | 7.24 ± 0.58 | 9.76 ± 0.66 | 3.65 ± 0.85 | 4 | 3 | 3.7 |
| 82 | 2.67 ± 0.26 | 3.36 ± 0.36 | 3.00 ± 0.77 | 10 | 8 | 4.5 |
| 83 | 2.82± 0.38 | 4.08 ± 0.36 | 4.31 ± 0.99 | 9 | 6 | 3.2 |
IC50 is the drug concentration effective in inhibiting 50% of the cell viability measured by WST-1 cell proliferation assay (WST-1) or trypan blue exclusion assay (TB) after 3 days exposure.
Human androgen-insensitive prostate cancer cell line
Human androgen-insensitive prostate cancer cell line
Human androgen-sensitive prostate cancer cell line