Journal ArticleDOI
Development of Organometallic Ruthenium−Arene Anticancer Drugs That Resist Hydrolysis
Wee Han Ang,Elisa Daldini,Claudine Scolaro,Rosario Scopelliti,Lucienne Juillerat-Jeannerat,Paul J. Dyson +5 more
Reads0
Chats0
TLDR
The new complexes were found to be highly soluble and kinetically more stable than their RAPTA precursor and showed a similar order of activity in inhibiting cancer cell-growth proliferation and exhibited oligonucleotide binding characteristics similar to those of the RAPT precursor, hence realizing a strategy for developing a new generation of stable and highly water-soluble RAPta adducts.Abstract:
With a view to develop drugs that could resist hydrolysis in aqueous media, organometallic arene-capped ruthenium(II) 1,3,5-triaza-7-phosphatricyclo[3.3.1.1]decane (RAPTA) complexes bearing chelating carboxylate ligands have been prepared and studied. The new complexes, Ru(η6-cymene)(PTA)(C2O4) (1) and Ru(η6-cymene)(PTA)(C6H6O4) (2), were found to be highly soluble and kinetically more stable than their RAPTA precursor that contains two chloride ligands in place of the carboxylate ligands. They were also able to resist hydrolysis in water and exhibited significantly lower pKa values. Importantly, they showed a similar order of activity in inhibiting cancer cell-growth proliferation (as determined by in vitro assays) and exhibited oligonucleotide binding characteristics (as evidenced by matrix-assisted laser desorption ionization mass spectrometry) similar to those of the RAPTA precursor, hence realizing a strategy for developing a new generation of stable and highly water-soluble RAPTA adducts.read more
Citations
More filters
Journal ArticleDOI
Organometallic Anticancer Compounds
TL;DR: The quest for alternative drugs to the well-known cisplatin and its derivatives, which are still used in more than 50% of the treatment regimes for patients suffering from cancer, is highly needed, and organometallic compounds have recently been found to be promising anticancer drug candidates.
Journal ArticleDOI
Bioorganometallic chemistry—from teaching paradigms to medicinal applications
TL;DR: In this tutorial review, various aspects of bioorganometallic chemistry are introduced, with the main emphasis on medicinal organometallic compounds, and rational ligand design has been shown.
Journal ArticleDOI
KP1019, a new redox-active anticancer agent--preclinical development and results of a clinical phase I study in tumor patients.
Christian G. Hartinger,Christian G. Hartinger,Michael A. Jakupec,Stefanie Zorbas-Seifried,Michael Groessl,Alexander E. Egger,Walter Berger,Haralabos Zorbas,Paul J. Dyson,Bernhard K. Keppler +9 more
TL;DR: The experimental evidence for the proposed mode of action of this coordination compound is discussed, including transport into the cell via the transferrin cycle and activation by reduction.
Journal ArticleDOI
Arene ruthenium complexes as anticancer agents
TL;DR: Neutral or cationic arene ruthenium complexes providing both hydrophilic as well as hydrophobic properties due to the robustness of the rUThenium-arene unit hold a high potential for the development of metal-based anticancer drugs.
Journal ArticleDOI
Stimuli-Responsive Therapeutic Metallodrugs.
TL;DR: This review presents a comprehensive and up-to-date overview on the therapeutic stimuli-responsive metallodrugs that have appeared in the past two decades, where stimuli such as redox, pH, enzyme, light, temperature, and so forth were involved.
References
More filters
Journal ArticleDOI
Rapid colorimetric assay for cellular growth and survival: Application to proliferation and cytotoxicity assays
TL;DR: A tetrazolium salt has been used to develop a quantitative colorimetric assay for mammalian cell survival and proliferation and is used to measure proliferative lymphokines, mitogen stimulations and complement-mediated lysis.
Journal ArticleDOI
An empirical method for correcting diffractometer data for absorption effects
N. Walker,David I. Stuart +1 more
TL;DR: In this article, a Fourier series in the polar angles of the incident and diffracted beam paths is used to model an absorption surface for the difference between the observed and calculated structure factors.
Journal ArticleDOI
Current status of platinum-based antitumor drugs.
Journal ArticleDOI
Ovarian cancer: strategies for overcoming resistance to chemotherapy
Roshan Agarwal,Stan B. Kaye +1 more
TL;DR: A better understanding of the mechanisms that underlie this drug resistance should allow treatment to be optimized, so that substantial improvements in the outlook for women with this disease can be achieved.