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.
Medicinal Chemistry
Title:Synthesis and Preliminary Biological Evaluation of Polyamine-aniline Acridines as P-glycoprotein Inhibitors
Volume: 10 Issue: 5
Author(s): Jianhong Wang, Pengfei Cheng, Tianwei Luo, Zhaoyi Wang, Yahong Zhang and Jin Zhao
Affiliation:
Keywords: Anilinoacridine derivatives, cytotoxicity, multidrug resistance, P-glycoprotein, polyamine.
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.
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Cite this article as:
Wang Jianhong, Cheng Pengfei, Luo Tianwei, Wang Zhaoyi, Zhang Yahong and Zhao Jin, Synthesis and Preliminary Biological Evaluation of Polyamine-aniline Acridines as P-glycoprotein Inhibitors, Medicinal Chemistry 2014; 10 (5) . https://dx.doi.org/10.2174/15734064113096660052
DOI https://dx.doi.org/10.2174/15734064113096660052 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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