Aims: A series of 8-methoxy ciprofloxacin- hydrazone/acylhydrazone hybrids were evaluated
for their activity against a panel of cancer cell lines including HepG2 liver cancer cells, MCF-7, doxorubicin-
resistant MCF-7 (MCF-7/DOX) breast cancer cells, DU-145 and multidrug-resistant DU145
(MDR DU-145) prostate cancer cells to seek for novel anticancer agents.
Background: Ciprofloxacin with excellent pharmacokinetic properties as well as few side effects, is one
of the most common used antibacterial agents. Notably, Ciprofloxacin could induce cancer cells apoptosis,
and cell cycle arrest at the S/G2 stage. The structure-activity relationship reveals that the introduction
of the methoxy group into the C-8 position of the fluoroquinolone moiety has resulted in a greater
binding affinity to the binding site, and 8-methoxy ciprofloxacin derivatives have proved a variety of
biological activities even against drug-resistant organisms. However, to the best of our current knowledge,
there are no studies that have reported the anticancer activity of 8-methoxy ciprofloxacin derivatives
so far. Furthermore, many fluoroquinolone-hydrazone/acylhydrazone hybrids possess promising
anticancer activity. Thus, it is rational to screen the anticancer activity of 8-methoxy ciprofloxacin derivatives.
Objective: To enrich the structure-activity relationship and provide new anticancer candidates for further
Methods: The desired 8-methoxy ciprofloxacin-hydrazone/acylhydrazone hybrids 5 and 6 were screened
for their in vitro anticancer activity against liver cancer cells HepG2, breast cancer cells MCF-7,
MCF7/DOX, prostate cancer cells DU-145 and MDR DU-145 by MTT assay.
Results: Some of 8-methoxy ciprofloxacin-hydrazone hybrids showed potential activity against HepG2,
MCF-7, MCF-7/DOX, DU-145 and MDR DU-145 cancer cell lines, low cytotoxicity towards VERO
cells and promising inhibitory activity on tubulin polymerization.
Conclusion: Compounds 5d and 5f showed promising anticancer activity, low cytotoxicity, and potential
tubulin polymerization inhibitory activity, were worthy of investigation.
Other: The structure-activity relationship was enriched.