Structure −Activity Relationship Studies of Targeting Ligands against Breast Cancer Cells

2009 ◽  
Vol 52 (21) ◽  
pp. 6744-6751 ◽  
Author(s):  
Nianhuan Yao ◽  
Wenwu Xiao ◽  
Leah Meza ◽  
Harry Tseng ◽  
Mathida Chuck ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity

Antiproliferative Activity of 8-methoxy Ciprofloxacin-Hydrozone/Acylhydrazone Scaffolds

2020 ◽  
Vol 20 (21) ◽  
pp. 1911-1915
Author(s):  
Li-Ping Wang ◽  
Zhi Xu ◽  
Gui-Ying Deng ◽  
Sha-Li Xu
Keyword(s):  
Anticancer Activity ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Prostate Cancer Cells ◽  
Liver Cancer Cells ◽  
Structure Activity ◽  
Low Cytotoxicity ◽  
Mcf 7

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.

Structure-activity relationships of resveratrol and derivatives in breast cancer cells

2009 ◽  
Vol 53 (7) ◽  
pp. 845-858 ◽  
Author(s):  
Rosamaria Lappano ◽  
Camillo Rosano ◽  
Antonio Madeo ◽  
Lidia Albanito ◽  
Pierluigi Plastina ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Structure Activity Relationships ◽  
Structure Activity
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