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Medicinal Chemistry
ISSN (Print): 1573-4064
ISSN (Online): 1875-6638
VOLUME: 10
ISSUE: 5
DOI: 10.2174/15734064113096660052      Price:  $58









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

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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.
Graphical Abstract:
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.