Issue 30, 2018, Issue in Progress

Synthesis and biological evaluation of novel quinolone derivatives dual targeting histone deacetylase and tubulin polymerization as antiproliferative agents

Abstract

A strategy to develop chemotherapy agents by combining two complimentary chemo-active groups into a single molecule may have higher efficacy and fewer side effects than that of single-target drugs. In this article, we describe the synthesis and evaluation of a series of novel dual-acting levofloxacin–HDACi conjugates to target both histone deacetylase (HDAC) and tubulin polymerization. These bifunctional conjugates exhibited potent inhibitory activities against HDACs and tubulin polymerization. In docking analysis provides a structural basis for HDACs inhibition activities. Moreover, these conjugates showed selective anticancer activity that is more potent against MCF-7 compared to other four cancer cells A549, HepG2, PC-3, HeLa, but they had no toxicity toward normal cells.

Graphical abstract: Synthesis and biological evaluation of novel quinolone derivatives dual targeting histone deacetylase and tubulin polymerization as antiproliferative agents

Supplementary files

Article information

Article type
Paper
Submitted
25 Mar 2018
Accepted
25 Apr 2018
First published
04 May 2018
This article is Open Access
Creative Commons BY license

RSC Adv., 2018,8, 16494-16502

Synthesis and biological evaluation of novel quinolone derivatives dual targeting histone deacetylase and tubulin polymerization as antiproliferative agents

X. Wang, X. Jiang, S. Sun and Y. Liu, RSC Adv., 2018, 8, 16494 DOI: 10.1039/C8RA02578A

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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