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Synthesis and Preliminary Biological Evaluation of Polyamine-aniline Acridines as P-glycoprotein Inhibitors

[ Vol. 10 , Issue. 5 ]

Author(s):

Jianhong Wang, Pengfei Cheng, Tianwei Luo, Zhaoyi Wang, Yahong Zhang and Jin Zhao   Pages 506 - 511 ( 6 )

Abstract:


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.

Keywords:

Anilinoacridine derivatives, cytotoxicity, multidrug resistance, P-glycoprotein, polyamine.

Affiliation:

Key Laboratory of Natural Medicines and Immunotechnology of Henan Province, Henan University, kaifeng 475004, Henan, P.R. China.

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