Gold complexes as potential anti-parasitic agents

Navarro, Maribel

doi:10.1016/j.ccr.2008.12.003

Cited by 211 publications

(72 citation statements)

References 89 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…At 10 µM, the effect of L1 did not result in CI decreases supporting the MTT findings where the IC 50 was reported to be > 100 µM (insert Fig 3). This finding also supports the fact that the activity/toxicity of the metal complex is as a result of the presence of the metal entity (Navarro 2009;Beraldo and Gambino 2004) which in addition to structurally stabilising the organic moiety or ligand (Navarro 2009), also improves activity.…”

Section: Rt-ces™ Findings Show Distinguishing Uptake and Recovery Patsupporting

confidence: 72%

Impedance technology reveals correlations between cytotoxicity and lipophilicity of mono and bimetallic phosphine complexes

et al. 2015

View full text Add to dashboard Cite

Label free impedance technology enables the monitoring of cell response patterns posttreatment with drugs or other chemicals. Using this technology, a correlation between the lipophilicity of metal complexes and the degree of cytotoxicity was observed. Au(L1)Cl (1), AuPd(L1)(SC 4 H 8 )Cl 3 (1a) and Au(L2)Cl (2) (L1 = (diphenylphosphino-2-pyridine); L2 = 2-(2-(diphenylphosphino)ethyl)-pyridine) were synthesised, in silico drug-likeness and structure activity relationship (SAR) monitored using impedance technology. Dose dependent changes in cytotoxicity were observed for the metal complexes resulting in IC 50s of 12.5±2.5, 18.3±8.3 and 16.9±0.5 µM for 1, 1a and 2 respectively in an endpoint assay. When a real time impedance assay was used, dose-dependent responses depicting patterns that suggested slower uptake (at a toxic 20 µM) and faster recovery of the cells (at the less toxic 10 µM) of the bimetallic complex (1a) compared to the monometallic complexes (1 and 2) was observed. These data agreed with the ADMET findings of lower aqueous solubility of 1a and non ideal lipophilicity (AlogP98 of 6.55) over more water soluble 1 and 2 with ideal lipophilicity (4.91 and 5.03 respectively) values. The additional coordination of a Pd atom to the nitrogen atom of a pyridine ring, the sulfur atom of a tetrahydrothiophene (THT) moiety and two chlorine atoms in 1a could be contributing to the observed differences when compared to the monometallic complexes. This report presents impedance technology as a means of 2 correlating drug-likeness of lipophilic phosphine complexes containing similar backbone structures and could prove valuable in filtering drug-like compounds in a drug discovery project.

show abstract

Section: Rt-ces™ Findings Show Distinguishing Uptake and Recovery Patsupporting

confidence: 72%

Impedance technology reveals correlations between cytotoxicity and lipophilicity of mono and bimetallic phosphine complexes

et al. 2015

View full text Add to dashboard Cite

show abstract

“…Neither metallic gold nor ligands had any appreciable inhibition on their own. The concept of metal-ligand synergism (Navarro 2009) therefore enhances activity as shown for the gold compounds.…”

Section: Discussionmentioning

confidence: 99%

“…The presence of the metal ion enhances the activity of the organic molecule. This is possibly due to the stabilization of the drug by coordination to the metal ion; a concept known as metal-drug synergism (Navarro 2009). Different metals such as platinum, vanadium (Sadler and Guo 1998;Sadler et al 1999;Suerbaum and Michetti 2002;Sun et al 2007), ruthenium, gold and rodium amongst many others have been shown to have medicinal properties when complexed with organic ligands.…”

Section: Introductionmentioning

confidence: 99%

HIV therapeutic possibilities of gold compounds

2010

View full text Add to dashboard Cite

Highly active antiretroviral therapy (HAART) has resulted in decreased mortality and morbidity from the acquired immune deficiency syndrome caused by the human immunodeficiency virus (HIV). Drug resistance and toxicity of HAART has led to the search for novel inhibitors of HIV infection. Gold-based compounds have shown promising activity against a wide range of clinical conditions and microorganism infections including HIV-1. A typical example is auranofin which resulted in an elevated CD4? T-cell count in an HIV patient being treated for psoriatic arthritis. In addition, reports exist on gold-based inhibitors of reverse transcriptase (RT), protease (PR) and viral entry of host cells. These and other characteristics of goldbased HIV drugs are reviewed here.

show abstract

“…This AuCl 3 (CTZ) complex (Fig. 3, middle) showed an anti-T. cruzi epomastigotes activity only slightly higher than the free CTZ (60 % vs. 58 %), with a poor performance compared other metal-CTZ complexes [36,40]. In another paper [38] (Fig.…”

Section: Nanogold Chemoterapymentioning

confidence: 99%

“…Navarro, who wrote a very interesting review in 2009 about gold complexes as potential anti-parasitic agents [40], published since 1997, together with different co-workers, also some papers in this series [35,36,38,39]. In one of those publications [36], the authors dealt with a group of metalclotrimazole complexes evaluating their activity against T. cruzi, including AuCl 3 (clotrimazole).…”

Section: Nanogold Chemoterapymentioning

confidence: 99%