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

ISSN: 1875-6638 (Online)
ISSN: 1573-4064 (Print)


Volume 10, 8 Issues, 2014


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Medicinal Chemistry

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Editor-in-Chief:
Atta-ur-Rahman, FRS
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Kings College
University of Cambridge
Cambridge
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Email: mc@benthamscience.org

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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 and Jin Zhao

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

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 Number: 5
First Page: 506
Last Page: 511
Page Count: 6
DOI: 10.2174/15734064113096660052
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