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

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.

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