Table 18.
In vitro and ex vivo anti-tumour activity by derivatives 13a and b: In in vitro tumour cell lines (monolayer assay) and in ex vivo human xenografts (clonogenic assay).
| Cell Line | IC50 a (μM) | Tumour Histotype |
IC50 a (μM) | ||
|---|---|---|---|---|---|
| 13a | 13b | 13a | 13b | ||
| Bladder | |||||
| BXF 1218L | 0.72 | 0.32 | BXF 1218 | 2.45 | 2.35 |
| BXF 1352L | 0.68 | 0.41 | BXF 1228 | 2.89 | 2.86 |
| BXF T24 | 1.72 | 0.58 | |||
| Lung Cancer | |||||
| LXFA 289L | 6.34 | 2.39 | LXFA 1012 | 4.76 | 27.34 |
| LXFA 526L | 1.57 | 0.67 | LXFA 1584 | 2.07 | 2.73 |
| LXFA 629L | 2.28 | 1.36 | LXFA 297 | 54.90 | >100 |
| LXFL 1121L | 0.67 | 0.38 | LXFA 526 | 2.96 | 3.15 |
| LXFL 529L | 1.85 | 0.67 | LXFA 629 | 2.23 | 3.63 |
| LXFL H460 | 2.08 | 0.89 | LXFA 677 | 23.19 | 27.02 |
| LXFA 923 | 19.50 | 25.68 | |||
| LXFE 1422 | 5.90 | 1.72 | |||
| LXFL 1072 | 3.44 | 3.42 | |||
| LXFL 529 | 5.07 | 4.46 | |||
| LXFL 625 | 24.04 | 38.21 | |||
| Colon Cancer | |||||
| CXF 269L | 1.39 | 0.56 | CXF 1103 | 4.47 | 18.36 |
| CXF HCT116 | 3.24 | 1.64 | CXF 1729 | 3.49 | 7.77 |
| CXF HT29 | 5.20 | 2.65 | CXF 1783 | 37.57 | 40.70 |
| CXF RKO | 1.50 | 0.63 | CXF 280 | 26.18 | 35.70 |
| CXF 975 | 6.93 | 6.03 | |||
| Head and Neck | |||||
| HNXF CAL27 | 0.81 | 0.50 | HNXF 536 | 2.45 | 2.67 |
| HNXF 908 | 2.57 | 4.00 | |||
| Melanoma | |||||
| MEXF 1341L | 0.52 | 0.19 | MEXF 1539 | 19.90 | 15.31 |
| MEXF 276L | 0.22 | 0.11 | MEXF 276 | 1.44 | 1.75 |
| MEXF 462NL | 1.31 | 0.55 | MEXF 462 | 3.24 | 4.10 |
| MEXF 989 | 1.18 | 0.58 | |||
| Ovarian Cancer | |||||
| OVXF OVCAR3 | 1.46 | 0.58 | OVXF 1353 | 20.96 | 22.90 |
| OVXF 899L | 5.40 | 2.03 | OVXF 899 | 3.54 | 3.93 |
| Renal Cancer | |||||
| RXF 1183L | 1.13 | 0.58 | RXF 1220 | 6.34 | 3.16 |
| RXF 1781L | 1.77 | 0.66 | RXF 486 | 2.90 | 3.90 |
| RXF 393NL | 3.14 | 1.34 | RXF 631 | 2.98 | 2.81 |
| RXF 486L | 3.86 | 1.60 | |||
| Prostate Cancer | |||||
| PRXF 22RV1 | 1.46 | 0.63 | PRXF DU145 | 28.67 | 25.98 |
| PRXF DU145 | 4.45 | 1.96 | PRXF PC3M | 2.89 | 2.80 |
| PRXF LNCAP | 2.10 | 0.68 | |||
| PRXF PC3M | 0.85 | 0.32 | |||
| Mammary Cancer | |||||
| MAXF 401NL | 1.24 | 0.64 | MAXF 1322 | 16.80 | 9.49 |
| MAXF MCF-7 | 2.44 | 0.98 | MAXF 1384 | 34.48 | 33.28 |
| MAXF MDA-231 | 1.18 | 0.49 | MAXF 401 | 5.90 | 11.32 |
| Gastric Cancer | |||||
| GXA MKN45 | 0.84 | 0.53 | GXF 1172 | 6.27 | >100 |
| GXF 251L | 1.56 | 0.65 | GXF 251 | 7.10 | 25.50 |
| GXF 97 | 2.72 | 3.74 | |||
| Pancreatic Cancer | |||||
| PANC1 | 0.74 | 0.41 | PAXF 546 | 3.52 | 14.63 |
| 1657L | 2.68 | 1.02 | PAXF 736 | 2.99 | 2.10 |
| 546L | 2.70 | 1.16 | |||
| Pleural mesothelioma | |||||
| PXF 1118L | 2.50 | 0.88 | PXF 1752L | 3.71 | 4.05 |
| PXF 1752L | 0.89 | 0.43 | PXF 541 | 2.20 | 0.37 |
| PXF 698L | 1.86 | 0.86 | |||
| Sarcoma | |||||
| SXF SAOS2 | 0.72 | 0.33 | SXF 1186 | 5.71 | 6.17 |
| SXF TE671 | 1.60 | 0.53 | SXF 1301 | 3.54 | 23.95 |
| SXF 627 | 3.40 | 4.06 | |||
| Uterus Cancer | |||||
| UXF 1138L | 0.72 | 0.35 | |||
a Concentration (μM) that inhibits 50% net cell growth.