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

Author(s): Jianhong Wang, Pengfei Cheng, Tianwei Luo, Zhaoyi Wang, Yahong Zhang, Jin Zhao.

Journal Name:Medicinal Chemistry

Volume 10 , Issue 5 , 2014

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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.

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Article Details

VOLUME: 10
ISSUE: 5
Year: 2014
Page: [506 - 511]
Pages: 6
DOI: 10.2174/15734064113096660052
Price: $58