Table 1.

Potency of FTC analogues for reversal of Bcrp1-mediated drug resistance

Values shown are EC90s, the concentration reversing 90% of Bcrp1-mediated drug resistance in MEF3.8/Bcrp1 clone A2 cells (IC50 for mitoxantrone = 42 + 4 nm, RF = 58 compared with parent MEF3.8 cells and the IC50 for topotecan = 1750 + 50 nm, RF = 36). The means are derived from eight repeats. All differences in potency between compounds were statistically significant by simple t test (P < 0.001).

CompoundMean EC90 (nm) ± SD
MitoxantroneTopotecan
Ko132190 ± 25270 ± 20
Ko13485 ± 10110 ± 10
Ko14323 ± 226 ± 5
GF12091851 ± 761 ± 8