Table 5. Testing of a Series of Representative STLC Analogues for the Inhibition of the MT-Stimulated ATPase Activity and in Human Leukemia (K562), Lung (NCI-H1299), Pancreas (BxPC3), and Colon (HCT116) Tumor Cell Lines and a Normal Breast Cell Line (hTERT-HME1).
| GI50 (nM) |
||||||
|---|---|---|---|---|---|---|
| compd | inhibition MT-stimulated ATPase activity, Kiapp (nM) | HCT116 | K562 | hTERT-HME1 | NCI-H1299 | BxPC-3 |
| 1 (STLC) | 143.8 ± 21.6 | 553 ± 57 | 1452 ± 76 | 361 ± 75 | 1549 ± 111 | 1563 ± 155 |
| 2 | 152.3 ± 15.0 | 1213 ± 40 | 2286 ± 213 | 1607 ± 199 | 2301 ± 511 | 2463 ± 908 |
| 3 (NSC123139) | 13.6 ± 2.4 | 130 ± 11 | 242 ± 22 | 57 ± 15 | 242 ± 28 | 284 ± 32 |
| 4 (NSC123529) | 4.2 ± 2.3 | 153 ± 10 | 247 ± 38 | 119 ± 3 | 227 ± 28 | 245 ± 43 |
| 5 (NSC123528) | 9.1 ± 2.2 | 130 ± 7 | 240 ± 17 | 81 ± 12 | 294 ± 24 | 291 ± 54 |
| rac-9 | 235.4 ± 47.5 | 828 ± 29 | 865 ± 131 | 494 ± 46 | 2825 ± 219 | 1489 ± 111 |
| (S)-9 | 384.4 ± 61.3 | 1603 ± 127 | 2065 ± 168 | 721 ± 99 | 4018 ± 303 | 4864 ± 545 |
| (R)-9 | 211.3 ± 24.6 | 472 ± 20 | 776 ± 26 | 321 ± 28 | 1324 ± 55 | 1119 ± 138 |
| 10 | 203.0 ± 44.5 | 213 ± 18 | 577 ± 61 | 572 ± 92 | 964 ± 214 | 1225 ± 296 |
| rac-29 | 5.1 ± 3.3 | 99 ± 5 | 91 ± 9 | 38 ± 7 | 137 ± 8 | 144 ± 6 |
| (R)-29 | 10.2 ± 2.0 | 51 ± 2 | 98 ± 12 | 26 ± 3 | 132 ± 7 | 75 ± 13 |
| (S)-29 | 12.8 ± 1.6 | 95 ± 7 | 128 ± 15 | 42 ± 5 | 281 ± 26 | 180 ± 35 |
| 30 | 10.8 ± 1.8 | 95 ± 5 | 200 ± 16 | 150 ± 32 | 360 ± 73 | 1211 ± 265 |
| 31 | 10.7 ± 3.6 | 230 ± 27 | 337 ± 28 | 308 ± 54 | 828 ± 37 | 2312 ± 418 |
| (R)-32 | 3.4 ± 1.6 | 40 ± 2 | 82 ± 4 | 27 ± 3 | 111 ± 6 | 85 ± 12 |
| (S)-32 | 19.3 ± 6.4 | 115 ± 6 | 149 ± 6 | 49 ± 4 | 305 ± 30 | 268 ± 27 |
| rac-32 | 9.8 ± 1.3 | 84 ± 6 | 98 ± 5 | 44 ± 4 | 204 ± 19 | 151 ± 29 |
| 33 | 9.7 ± 1.8 | 154 ± 7 | 233 ± 21 | 601 ± 107 | 376 ± 37 | 1603 ± 168 |
| 54 (ispinesib) | 2.5 ± 1.2 | 25 ± 3 | 71 ± 8 | 32 ± 8 | 82 ± 10 | 80 ± 15 |