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

Table 11.

Reversal effects of sesquiterpene 100 and its derivatives 101–105 of P-gp-mediated daunomycin resistance on NIH-3T3MDR1 G-185 murine cells [129].

graphic file with name molecules-25-03364-i035.jpg

Compound R1 R2 Activity
Ki 1 (µM) RF 2 (Daunomycin) RF 2 (Vimblastine)
100 OH OH 0.28 5.6 23.7
101 OH graphic file with name molecules-25-03364-i036.jpg 0.54 10.8 19.1
102 OH graphic file with name molecules-25-03364-i037.jpg 0.13 11.8 17.4
103 OH graphic file with name molecules-25-03364-i038.jpg 1.21 11.8 11.2
104 OH graphic file with name molecules-25-03364-i039.jpg 0.19 15.8 27.4
105 graphic file with name molecules-25-03364-i040.jpg OH 0.63 10.0 20.6
Verapamil (1) - - 2.8 8.7

1 Ki—concentration of compounds that inhibits 50% of P-gp-mediated daunomycin transport; 2 RF—Reversal fold: indicate the ability of the tested compounds to reduce resistance of multidrug resistance cells to daunomycin/vinblastine. RF values were calculated by the ratio between IC50 of daunomycin or vinblastine in the absence and in the presence of the tested sesquiterpene derivatives at 1 µM.