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Inhibition of human topoisomerase I and anti-proliferative effects on MCF-7 cells by new titanocene complexes
- Publication Year :
- 2015
-
Abstract
- The antitumor activity shown by many platinum complexes has produced a strong interest in research of new organometallic compounds having anticancer action. Among the many metal compounds synthesized and tested, those based on titanium have received considerable attention because of their cytotoxic activity against solid tumors. Particularly, new titanocene compounds containing aromatic groups linked to the Cp (cyclopentadienyl ring, C5H5) have been synthetized, such as the titanocene Y (bis-[(p-methoxybenzyl)cyclopentadienyl]titanium dichloride) that displayed promising medium-high cytotoxic activity on breast cancer cell lines. Other titanocene complexes recently synthesized, obtained by replacing the substituent methoxy-aryl of cyclopentadienes of titanocene Y with ethenyl-methoxide or ethenyl-phenoxide, showed increased cytotoxic activity on breast cancer cell lines being more stable compounds. In this paper, we report that new titanocene complexes holding lipophilic groups, for instance a methyl group on benzyl carbon, exhibit improved antiproliferative effect on breast cancer cell line MCF-7. Similar results have been obtained introducing a 5-methoxy naphthyl group to further stabilize the titanocene complexes. These inhibitory effects on breast cancer cells have been ascribed to human topoisomerase I and II inhibition as demonstrated by specific enzymatic assays.
- Subjects :
- Stereochemistry
Cell Survival
Clinical Biochemistry
Substituent
Pharmaceutical Science
topoisomerasi I
Topoisomerase-I Inhibitor
Biochemistry
chemistry.chemical_compound
Cyclopentadienyl complex
Antigens, Neoplasm
Drug Discovery
Organometallic Compounds
Cytotoxic T cell
Humans
Topoisomerase II Inhibitors
Molecular Biology
biology
Chemistry
Topoisomerase
titanocene complexes
Organic Chemistry
DNA-Binding Proteins
DNA Topoisomerases, Type II
MCF-7
DNA Topoisomerases, Type I
Microscopy, Fluorescence
biology.protein
MCF-7 Cells
Molecular Medicine
Topoisomerase-II Inhibitor
Topoisomerase I Inhibitors
Methyl group
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Accession number :
- edsair.doi.dedup.....0dc5e0fb96db51600ccb91bfe64d148c