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. 2020 Jul 24;25(15):3364. doi: 10.3390/molecules25153364

Table 7.

P-gp modulating activity of flavone derivatives 80–84 on K562/DOX cells [114].

graphic file with name molecules-25-03364-i020.jpg

Compound R1 R2 R3 [I]0.5 (µM) 1 αmax 2
80 (CH2)5 CH3 OH 0.96 0.99
81 (CH2)5 CH3 H 0.34 0.99
82 (CH2)5 graphic file with name molecules-25-03364-i021.jpg H 0.43 0.99
83 (CH2)5 H H 1.32 0.69
84 (CH2)2O(CH2)2 CH3 H 1.23 0.86
Verapamil (1) - - - 1.60 0.70

1 [I]0.5 represents the concentration that causes a half-maximal increase (a = 0.5) in the nuclear concentration of pirarubicin and measures the potency of the modulator. Lower [I]0.5 values mean stronger P-gp modulators; 2 αmax represents the efficacy of the modulator and is the maximum increase in the nuclear concentration of pirarubicin in resistant cells that can be obtained with a given compound. The value of αmax varies between 0 (in the absence of the inhibitor) and 1 (when the amount of pirarubicin in resistant cells is the same as in sensitive cells).