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 investigations.

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.

目的：评估了一系列8-甲氧基环丙沙星/酰基hydr杂化物对一组癌细胞系的活性，这些癌细胞系包括HepG2肝癌细胞，MCF-7，抗阿霉素的MCF-7（MCF-7 / DOX）乳腺癌癌细胞，DU-145和多药耐药性DU145（MDR DU-145）前列腺癌细胞，以寻求新型抗癌药。

背景：环丙沙星具有优异的药代动力学特性，且副作用极少，是最常用的抗菌剂之一。值得注意的是，环丙沙星可以诱导癌细胞凋亡，并在S / G2期抑制细胞周期。结构-活性关系表明，将甲氧基引入氟喹诺酮部分的C-8位导致对结合位点的结合亲和力更大，并且8-甲氧基环丙沙星衍生物已证明具有多种生物学活性，即使对耐药生物。然而，就我们目前所知，迄今尚无研究报道8-甲氧基环丙沙星衍生物的抗癌活性。此外，许多氟喹诺酮-/酰基hydr杂化物具有有希望的抗癌活性。从而，

目的：丰富构效关系，为进一步的研究提供新的候选抗癌药物。

方法：筛选所需的8-甲氧基环丙沙星hydr /酰基hydr杂化物5和6对肝癌细胞HepG2，乳腺癌细胞MCF-7，MCF7 / DOX，前列腺癌细胞DU-145和MDR DU的体外抗癌活性。通过MTT测定法测定-145。

结果：一些8-甲氧基环丙沙星-杂化物对HepG2，MCF-7，MCF-7 / DOX，DU-145和MDR DU-145癌细胞系具有潜在活性，对VERO细胞的细胞毒性低，并且对微管蛋白具有抑制作用聚合。

结论：化合物5d和5f具有良好的抗癌活性，低细胞毒性和潜在的微管蛋白聚合抑制活性，值得研究。

其他：结构-活性关系得到了丰富。