TABLE 1.
Cytotoxicity of ligustrazine–heterocyclic derivatives (TMPH) to five kinds of cells by MTT assay.
| TMPH | Antiproliferative activity IC50 ± SEM (µM) | |||||
|---|---|---|---|---|---|---|
| MCF-7 | MDA-MB-231 | 4T1 | L929 | HUVEC | SI | |
| 8–1 | 10.99 ± 0.06 | 2.52 ± 0.08 | >20 | 16.58 ± 0.12 | >20 | 6.58 |
| 8–2 | 6.62 ± 0.15 | 6.10 ± 0.16 | 19.86 ± 0.16 | >20 | 4.27 ± 0.07 | >3.28 |
| 8–3 | 4.15 ± 0.02 | 3.39 ± 0.12 | 19.47 ± 0.45 | 4.12 ± 0.32 | 9.78 ± 0.05 | 1.22 |
| 8–4 | 6.21 ± 0.14 | 5.77 ± 0.09 | >20 | 10.70 ± 0.43 | >20 | 1.85 |
| 8–5 | 4.96 ± 0.25 | 3.44 ± 0.16 | 2.07 ± 0.04 | 3.49 ± 0.28 | >20 | 1.01 |
| 8–6 | >20 | 1.02 ± 0.15 | 1.94 ± 0.03 | >20 | >20 | >19.61 |
| 8–9 | >20 | 8.45 ± 0.14 | 3.74 ± 0.19 | >20 | >20 | >2.37 |
| 8–10 | 2.84 ± 0.21 | 6.67 ± 0.16 | 2.48 ± 0.24 | 5.48 ± 0.06 | 4.54 ± 0.01 | 0.82 |
| 8–11 | >20 | 5.05 ± 0.02 | 11.95 ± 0.46 | >20 | 10.35 ± 0.03 | >3.96 |
| 8–12 | 5.38 ± 0.13 | 11.24 ± 0.12 | 10.25 ± 0.32 | >20 | >20 | >1.78 |
| 8–13 | >20 | 2.44 ± 0.09 | 13.68 ± 0.24 | 15.67 ± 0.36 | 14.40 ± 0.03 | 6.42 |
| 10–1 | 2.61 ± 0.19 | 1.14 ± 0.08 | 2.86 ± 0.18 | 4.36 ± 0.37 | >20 | 3.82 |
| 10–2 | 4.19 ± 0.15 | 8.41 ± 0.18 | >20 | 11.66 ± 0.81 | 16.63 ± 0.68 | 1.39 |
| 10–3 | 18.54 ± 1.34 | 4.16 ± 0.25 | 17.55 ± 1.16 | 7.26 ± 0.16 | >20 | 1.75 |
| 10–4 | >20 | 13.02 ± 0.27 | >20 | >20 | >20 | >1.54 |
| 10–5 | 8.72 ± 0.49 | 5.76 ± 0.13 | >20 | 5.18 ± 0.27 | >20 | 0.90 |
| 10–6 | 6.49 ± 0.36 | 7.76 ± 0.14 | 11.98 ± 0.54 | 8.91 ± 0.12 | 10.21 ± 0.86 | 1.15 |
| 10–9 | 3.37 ± 0.19 | 6.01 ± 0.11 | 3.12 ± 0.14 | 7.37 ± 0.57 | 9.63 ± 0.53 | 1.23 |
| 10–10 | 2.93 ± 0.05 | 2.83 ± 0.09 | >20 | 10.13 ± 0.52 | 11.16 ± 0.38 | 3.58 |
| 10–11 | 3.23 ± 0.03 | 12.89 ± 1.41 | >20 | >20 | >20 | >1.55 |
| 10–12 | 2.86 ± 0.08 | 3.41 ± 0.12 | >20 | >20 | >20 | >5.87 |
| 10–13 | 3.09 ± 0.13 | 4.60 ± 0.29 | 9.88 ± 0.22 | 12.64 ± 0.12 | 10.51 ± 1.24 | 2.75 |
| 12–1 | 1.95 ± 0.06 | 2.78 ± 0.37 | 2.66 ± 0.05 | 4.75 ± 0.26 | 13.17 ± 1.12 | 1.71 |
| 12–2 | 2.71 ± 0.07 | 3.38 ± 0.12 | 3.97 ± 0.01 | 3.78 ± 0.14 | 10.96 ± 0.68 | 1.12 |
| 12–3 | 3.26 ± 0.16 | 2.12 ± 0.06 | 5.13 ± 0.28 | 7.65 ± 0.06 | 7.86 ± 0.01 | 3.61 |
| 12–4 | 3.23 ± 0.18 | 3.52 ± 0.12 | 6.62 ± 0.14 | >20 | >20 | >5.68 |
| 12–5 | 1.36 ± 0.06 | 2.39 ± 0.12 | 3.50 ± 0.06 | 4.18 ± 0.05 | 11.36 ± 0.44 | 1.75 |
| 12–6 | 2.04 ± 0.03 | 1.98 ± 0.15 | 4.18 ± 0.09 | 5.35 ± 0.17 | 7.03 ± 0.05 | 2.70 |
| 12–9 | 1.11 ± 0.15 | 0.84 ± 0.02 | 1.16 ± 0.18 | 3.16 ± 0.13 | 3.82 ± 0.24 | 3.76 |
| 12–10 | 2.09 ± 0.06 | 2.42 ± 0.06 | 1.63 ± 0.03 | 3.82 ± 0.07 | 12.37 ± 0.09 | 1.58 |
| 12–11 | 1.76 ± 0.02 | 2.42 ± 0.18 | 2.32 ± 0.14 | >20 | >20 | >8.26 |
| 12–12 | 2.21 ± 0.15 | 1.64 ± 0.12 | 2.69 ± 0.04 | 18.86 ± 0.44 | 12.16 ± 0.20 | 11.50 |
| 12–13 | 1.61 ± 0.08 | 5.01 ± 0.16 | 4.76 ± 0.45 | 8.89 ± 0.12 | 10.70 ± 1.06 | 1.77 |
| TMP | >20 | >20 | >20 | >20 | >20 | NC |
| DDP | 6.25 ± 0.34 | 3.18 ± 0.06 | 5.71 ± 0.16 | 8.38 ± 0.23 | 7.46 ± 0.45 | 2.64 |
SI, selectivity index; SI = IC50 (L929)/IC50 (MDA-MB-231); NC, not calculated.