Medical uses of gold compounds: Past, present and future

Pricker, Simon P

doi:10.1007/bf03215464

Cited by 254 publications

(184 citation statements)

References 23 publications

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“…Scheme 1 Gold(I) complexes of imidazolate (1)(2)(3)(4)(5), pyrazolate (5-9), 1,2,3-triazolate (10-14), 1,2,4-triazolate (15-18) and pyrrolate (19).…”

Section: List Of Figure Captionsmentioning

confidence: 99%

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Amides of gold(I) diphosphines prepared from N-heterocyclic sources and their in vitro and in vivo screening for anticancer activity

Horvath

Dobrzańska

Strasser

et al. 2012

Journal of Inorganic Biochemistry

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Synopsis __________________________________________________________________________Among a new series of gold(I) complexes that contain diphosphine and deprotonated N-heterocyclic ring systems as ligands, the compounds containing diphenyl(phosphino)pentane and pyrazolate (lypophilic) or 1,2,4,-triazolate (hydrophilic) have high anti-tumour specificities. They induce an apoptic cell death pathway and have the maximum tolerated dose of 1.5 μmol/kg when administered to Balb/C mice. ___________________________________________________________________ *Synopsis for the Graphical abstract  In 25 new complexes diphosphines and azolate-type ligands coordinate to gold  Solvent molecules and counterions appear within channels of a crystalline complex  Cytotoxicity is dependent upon aliphatic C chain length in the ligands  An apoptosis cell death with certain mitochondrial involvement is indicated  Tolerated doses compared to [Au(dppe) 2 ]Cl, tumour specificity is much better *Highlights A B S T R A C T ------------------------------------------------------------------------A series of new neutral mononuclear or dinuclear gold(I) complexes and a cyclic cationic tetranuclear amidogold(I) complex comprising of the phosphines 1,2-bis(dimethylphosphino)ethane (dmpe), μ-1,2-bis(diphenylphosphino)ethane (dppe), μ-1,3-bis(diphenylphosphino)propane (dppp), μ-1,5-bis(diphenylphosphino)pentane (dpppe), μ-1,6-bis(diphenylphosphino)hexane (dpph) or trimethylphosphine, and several N-heterocyclic ring systems (imidazolate, pyrazolate, 1,2,3-triazolate, 1,2,4-triazolate, pyrrolate, 9H-purine-9-ate or 9H-purine-6-amine-9-ate) as ligands, reveal intermolecular aurophilic interactions and 2D channels available for solvent molecules in some of their crystal structures. The antitumou r 2 activity of the acyclic gold(I) compounds is highly dependent on the substituents on the phosphorus atoms being highest for phenyl groups and lower for methyl groups. The activity of these compounds against selected cell lines is linked to the length of the carbon bridge between the two phosphorus atoms being highest with a bridge consisting of 5 or 6 carbons. Two compounds with the highest tumour specifities that contain dpppe and pyrazolate (a lipophilic compound) or 1,2,4-triazolate (a hydrophilic compound) induce the apoptic cell death pathway and tolerate a maximum dose of 1.5 μmol/kg when administered to Balb/C mice.

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“…Scheme 1 Gold(I) complexes of imidazolate (1)(2)(3)(4)(5), pyrazolate (5-9), 1,2,3-triazolate (10-14), 1,2,4-triazolate (15-18) and pyrrolate (19).…”

Section: List Of Figure Captionsmentioning

confidence: 99%

“…The pharmacological application of gold(I) compounds in the treatment of rheumat oid arthritis and their potential activity as anticancer, antiviral and antimicrobial agents has provided a powerful incentive for the continued interest in the bonding of biologically active molecules to gold(I) [1][2][3][4][5].…”

Section: Introductionmentioning

confidence: 99%

Amides of gold(I) diphosphines prepared from N-heterocyclic sources and their in vitro and in vivo screening for anticancer activity

Horvath

Dobrzańska

Strasser

et al. 2012

Journal of Inorganic Biochemistry

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“…Gold-based drugs, very well known for rheumatoid arthritis (RA) treatment [2,3], also demonstrate anti-HIV activity, reviewed by Fonteh et al, 2010 [4]. Ligands play a crucial role in the synthesis of gold-based compounds in that their complexation to metals not only gives rise to stable compounds, but in some cases leads to better activities and/or didanosine boosts immune parameters including increases in CD4+ cell count [20].…”

Section: Introductionmentioning

confidence: 99%

New bis(thiosemicarbazonate) gold(III) complexes inhibit HIV replication at cytostatic concentrations: Potential for incorporation into virostatic cocktails

Fonteh

Keter

Meyer

2011

Journal of Inorganic Biochemistry

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“…This is due to the fact that gold(I) is thermodynamically more stable than gold (III) with most gold(III) complexes being strong oxidizing agents which are easily reduced to gold(I). Biologically occurring reductants such as thiols reduce gold(III) to gold(I), making gold(III) compounds generally very toxic (Fricker 1996a). That notwithstanding, there is evidence of gold(III) compounds with anti-HIV activity and limited toxicity (Sun et al 2004;.…”

Section: Introductionmentioning

confidence: 99%

HIV therapeutic possibilities of gold compounds

2010

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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.

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Medical uses of gold compounds: Past, present and future

Cited by 254 publications

References 23 publications

Amides of gold(I) diphosphines prepared from N-heterocyclic sources and their in vitro and in vivo screening for anticancer activity

Amides of gold(I) diphosphines prepared from N-heterocyclic sources and their in vitro and in vivo screening for anticancer activity

New bis(thiosemicarbazonate) gold(III) complexes inhibit HIV replication at cytostatic concentrations: Potential for incorporation into virostatic cocktails

HIV therapeutic possibilities of gold compounds

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