Table 1. Cytotoxicity of the Compounds (Chemical Structures in Figure 1) in Ovarian Tumor Cell Lines Sensitive to MSA (A2780) and MSA-Resistant due to P-gp Overexpression (A2780AD) and in Cervical Tumor Cell Lines Sensitive to MSA (HeLa S3) and MSA-Resistant due to βIII-Tubulin Overexpression (HeLa-βIII).
compound | A2780 (nM) | A2780AD (nM) | R/S | HeLa-S3 (nM) | HeLa βIII (nM) | R/S | Crb (μM) |
---|---|---|---|---|---|---|---|
dimethyl sulfoxide (DMSO, vehicle) | 3.3 ± 0.1a | ||||||
paclitaxel | 1.8 ± 0.4 | 1491 ± 284 | 828.2 | 0.8 ± 0.2 | 8.6 ± 1.4 | 10.8 | 0.5 ± 0.1a |
dictyostatin | 2.55 ± 1 | 3.9 ± 0.2 | 1.5 | 1.5 ± 0.3 | 4.4 ± 0.8 | 2.9 | 0.4 ± 0.1 |
2 | 1203 ± 52 | 1423 ± 39 | 1.2 | 1050 ± 145 | 1160 ± 115.2 | 1.1 | 3.3 ± 0.3 |
discodermolide | 28 ± 3 | 37.9 ± 5.2 | 1.35 | 6 ± 0.8 | 13.2 ± 1.25 | 2.2 | 0.6 ± 0.1 |
4 | 3.6 ± 1.5 | 5.1 ± 0.85 | 1.4 | 3.5 ± 0.7 | 10.2 ± 1.5 | 3.0 | 1.2 ± 0.1 |
5 | 5.5 ± 1.2 | 4.7 ± 1.6 | 0.85 | 9.7 ± 1.9 | 35 ± 2 | 3.6 | 1.4 ± 0.1 |
6 | 33.3 ± 11.6 | 16 ± 0.7 | 0.5 | 13 ± 3 | 18.5 ± 1.1 | 1.4 | 2.2 ± 0.2 |
7 | 7000 ± 300 | 8575 ± 125 | 1.2 | 2627.5 ± 182 | 7275 ± 625 | 2.8 | 3.4 ± 0.2 |
8 | 30.6 ± 8.2 | 17.6 ± 0.45 | 0.6 | 16.7 ± 3.2 | 15.3 ± 1.4 | 0.9 | 2.4 ± 0.1 |
9 | 4.9 ± 0.8 | 6.9 ± 0.4 | 1.4 | 1.9 ± 0.1 | 6.15 ± 0.8 | 3.2 | 0.5 ± 0.1 |
10 | 42.95 ± 4.7 | 94.4 ± 2.7 | 2.2 | 18.3 ± 1.9 | 21 ± 1.5 | 1.2 | 1.4 ± 0.2 |
11 | 66.6 ± 8.9 | 260 ± 43 | 3.9 | 25.85 ± 1.3 | 31.35 ± 4 | 1.2 | 0.8 ± 0.1 |
12 | 1.9 ± 0.9 | 0.9 ± 0.1 | 0.5 | 0.5 ± 0.02 | 1.8 ± 0.2 | 3.6 | 1.1 ± 0.1 |
13 | 69 ± 1.7 | 413.5 ± 21.6 | 6 | 32.6 ± 4.65 | 31.2 ± 6.5 | 1.0 | 1.2 ± 0.1 |
14 | 101.5 ± 3.95 | 89.3 ± 3.9 | 0.9 | 34 ± 3 | 67 ± 5.4 | 1.9 | 1.5 ± 0.2 |
15 | 488 ± 35 | 551.5 ± 53.3 | 1.1 | 719 ± 39 | 1047.5 ± 120 | 1.5 | 0.9 ± 0.1 |
16 | 2933 ± 219 | 4733 ± 437 | 1.6 | 2360 ± 133 | 1450 ± 104.1 | 0.6 | 1.8 ± 0.1 |
Data taken from ref (3).
Cr for tubulin assembly in the GAB buffer.