Acute renal failure (ARF) is a deleterious condition with increased mortality or healthcare costs dialysis-dependent end-stage disease. The study aims to compare prophylaxis fondaparinux (Fund) vs. treatment alteplase (Alt) in ameliorating cisplatin (Cis)-induced ARF. Sixty male mice were equally divided randomly into six groups of control, Cis, Alt, and Cis + Alt receiving normal saline for 10...

We have investigated the processing of site-specific Pt-DNA cross-links in live mammalian cells to enhance our understanding of the mechanism of action of platinum-based anticancer drugs. The activity of platinum drugs against cancer is mediated by a combination of processes including cell entry, drug activation, DNA-binding, and transcription inhibition. These drugs bind nuclear DNA to form Pt...

A simple method for the preparation of cis-dichloro(1,4,7-triazacyclononane)platinum(II), cis-Pt(tacn)Cl(2) is presented, together with the results of screening the compound against the K-562 (leukemia) and SK-OV-3 (ovarian) human cancer cell lines. While the compound shows no activity against K-562 cells, there is evidence for some cytotoxicity against SK-OV-3. The compound is much less effect...

Mixed amine/ammine motifs are important features in newer generation platinum anticancer agents, including the Pt(IV) prodrug satraplatin. One synthetic route that can be used to access platinum molecules with such structures exploits the trans effect during NH3-mediated cleavage of iodo-bridged platinum(II) dimers of the form [Pt(Am)I(μ-I)]2, where Am is an amine. A clear picture of the nature...

The ternary complexes of formulae cis-[(NH(3))(2)Pt(nucl)(amac)]NO(3), where nucl = guo and cyd (guanosine and cytidine) and amac = the deprotonated aminoacids glycine (gly), L-alanine (ala), L-2-aminobutyric acid (2-aba), L-norvaline (nval) and L-norleucine (nleu), were prepared from the reactions of the binary chelated ones cis-[(NH(3))(2)Pt(nucl)(amac)]NO(3) with the nucleosides.They were ch...

The kinetics of chloride substitution from a series of square-planar platinum(II) complexes, viz. [Pt(terpyridine)Cl](+), (Pt1), [Pt{2-(2'-pyridyl)-1,10-phenanthroline}Cl]Cl, (Pt2), [Pt{4'-(2'''-CH3-phenyl)-2,2':6',2''-terpyridine}Cl]CF3SO3 (Pt3) and [Pt{4'-(2'''-CH3-phenyl)-6-(3''-isoquinoyl)-2,2'bipyridine}Cl]SbF6 (Pt4) were studied using a series of five-membered heterocyclic neutral nitroge...

Cytotoxicity assays of azolato-bridged dinuclear Pt(II) complexes, [{cis-Pt(NH(3))(2)}(2)(μ-OH)(μ-azolato)](2+), where the azolato was pyrazolato (1), 1,2,3-triazolato-N1,N2 (2), tetrazolato-N1,N2 (3), or tetrazolato-N2,N3 (4), were performed in cisplatin-sensitive and -resistant human non-small-cell lung cancer cell lines (PC-9 and PC-14). These complexes largely circumvented the cisplatin res...

The primary objective was to understand more deeply the molecular mechanism underlying different antitumor effects of dinuclear Pt(II) complexes containing aromatic linkers of different length, {[cis-Pt(NH(3))(2)Cl](2)(4,4'-methylenedianiline)}(2+) (1) and {[cis-Pt(NH(3))(2)Cl](2)(alpha,alpha'-diamino-p-xylene)}(2+) (2). These complexes belong to a new generation of promising polynuclear platin...

Platinum(iv) complexes take advantage of the exclusive conditions that occur within the tumor to carry out their cytotoxic activity. On the other hand, silk fibroin has natural properties which make it very interesting as a biomaterial: high biocompatibility, biodegradability, low immunogenicity, high cellular penetration capacity and high reactive surface. Herein we report the preparation of s...

Cisplatin (cis-[Pt(NH3)2Cl2]) is a widely used antitumor agent whose mutagenic activity raises the possibility of the induction of secondary cancer as a result of treatment. Mutation of the proto-oncogene H-ras is found in more than 30% of all human tumors, where it has been postulated to contribute to the initiation and progression of human cancers. Activating mutations in the H-ras gene are p...