Synthesis and Preliminary Biological Evaluation of Polyamine-aniline Acridines as P-glycoprotein Inhibitors
Jianhong Wang, Pengfei Cheng, Tianwei Luo, Zhaoyi Wang, Yahong Zhang and Jin Zhao
Affiliation: Key Laboratory of Natural Medicines and Immunotechnology of Henan Province, Henan University, kaifeng 475004, Henan, P.R. China.
Keywords: Anilinoacridine derivatives, cytotoxicity, multidrug resistance, P-glycoprotein, polyamine.
We have synthesized a series of polyamine-based anilinoacridine derivatives. The preliminary biological
evaluation indicated that the 9-anilinoacridine-polyamine derivatives had low or insignificant in vitro cytotoxicity against
K562 cell line and K562/ADM, the drug-resistant cell line. However, the evaluation for P-gp modulation showed that they
held potent P-gp inhibitory ability. Among them, the effect of compound 7c on P-gp was even greater than that of Verapamil,
the known P-gp modulator. The results suggest that 9-anilinoacridine-polyamine derivatives can be employed as
effective P-gp modulators.
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