Novel organometallic cationic ruthenium(II) pentamethylcyclopentadienyl benzenesulfonamide complexes targeted to inhibit carbonic anhydrase
| Autor: | Peter G. Parsons, Sally-Ann Poulsen, Peter Conrad Healy, Claudiu T. Supuran, Michael Lloyd Williams, Bradley Thomas Loughrey, Daniela Vullo, Alessio Innocenti |
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| Rok vydání: | 2009 |
| Předmět: |
Stereochemistry
Cell Survival chemistry.chemical_element Biochemistry Isozyme Ruthenium Inorganic Chemistry Inhibitory Concentration 50 Carbonic anhydrase Cell Line Tumor Organometallic Compounds Animals Humans Cytotoxicity Carbonic Anhydrase Inhibitors Carbonic Anhydrases chemistry.chemical_classification Sulfonamides biology Cationic polymerization In vitro Enzyme chemistry Cell culture biology.protein |
| Zdroj: | Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry. 14(6) |
| ISSN: | 1432-1327 |
| Popis: | Cationic ruthenium(II) pentamethylcyclopentadienyl benzenesulfonamide sandwich complexes have been synthesized and screened for enzymatic inhibition of the physiologically dominant carbonic anhydrase (CA) isozymes: human CA I and II, mitochondrial isozymes VA and VB, and the cancer-associated isozyme IX. The complexes demonstrated weaker binding to CAs compared with typical aromatic sulfonamides, inhibiting the enzyme at high nanomolar concentrations. An in vitro cytotoxic evaluation of the complexes was also undertaken against a range of tumorigenic cell lines and a healthy human cell line. Complexes inhibited the growth of cancerous cells at low micromolar concentrations while expressing lower levels of toxicity towards the normal human cell line. Factors influencing the synthesis, cytotoxicity, and enzyme affinity for this series of organometallic complexes are discussed. |
| Databáze: | OpenAIRE |
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