Table 1.
EC50 (nM) of FD18 metabolites in reversing P-gp mediated MDR.
| Compounds | |||||
|---|---|---|---|---|---|
| FD18 | 14a (M1) | FM04 (M2) | FM327 (M3) | ||
| EC50 (nM) needed for reversing MDR in LCC6MDR cells | PTX | 148 ± 18 a | 305 ± 35 a | 83 ± 7 | >1000 |
| Vinblastine | 173 ± 27 a | ND | 61 ± 13 | ND | |
| Vincristine | 179 ± 32 a | ND | 83 ± 11 | ND | |
| DOX | 131 ± 13 a | ND | 153 ± 39 | ND | |
| Daunorubicin | 95 ± 25 a | ND | 88 ± 52 | ND | |
| Mitoxantrone | 90 ± 20 a | ND | 64 ± 27 | ND | |
| Physicochemical properties | Molecular Weight | 724 | ND | 415 | ND |
| CLogP | 9.0 | ND | 4.9 | ND | |
| tPSA (Å2) | 92.8 | ND | 56.8 | ND | |
Effective concentration (EC50) was a concentration of modulator at which the IC50 of an anticancer drug can be reduced by half in the LCC6MDR cells. a EC50 values of FD18 or 14a for reversing MDR in LCC6MDR cells had been published in 2012 [23]. They were included here for comparison. Molecular weight, CLogP and tPSA were compared for FD18 and FM04. The CLogP and tPSA were analyzed using ChemDraw Ultra 12.0 software. The EC50 values were presented as mean ± standard error of the mean. N = 3–7 independent experiments. ND = not determined.