ChloroquineV1, Main, Exploration, bibRecord, 001A76

Development of Ruthenium Antitumor Drugs that Overcome Multidrug Resistance Mechanisms

Identifieur interne : 001A76 ( Main/Exploration ); précédent : 001A75; suivant : 001A77

Development of Ruthenium Antitumor Drugs that Overcome Multidrug Resistance Mechanisms

Auteurs : Carsten A. Vock [Italie] ; Wee Han Ang [Italie] ; Claudine Scolaro [Italie] ; Andrew D. Phillips [Italie] ; Lucienne Lagopoulos [Italie] ; Lucienne Juillerat-Jeanneret [Italie, Suisse] ; Gianni Sava [Italie] ; Rosario Scopelliti [Italie] ; Paul J. Dyson [Italie, Suisse]

Source :

Journal of Medicinal Chemistry [ 0022-2623 ] ; 2007.

RBID : ISTEX:C870BF311561AE6669884B025335064C04D8FE7E

Abstract

Organometallic ruthenium(II) complexes of the general formula [Ru(η6-p-cymene)Cl2(L)] and [Ru(η6-p-cymene)Cl(L)2][BPh4] with modified phenoxazine- and anthracene-based multidrug resistance (MDR) modulator ligands (L) have been synthesized, spectroscopically characterized, and evaluated in vitro for their cytotoxic and MDR reverting properties in comparison with the free ligands. For an anthracene-based ligand, coordination to a ruthenium(II) arene fragment led to significant improvement of cytotoxicity as well as Pgp inhibition activity. A similar, but weaker effect was also observed when using a benzimidazole-phenoxazine derivative as Pgp inhibitor. The most active compound in terms of both Pgp inhibition and cytotoxicity is [Ru(η6-p-cymene)Cl2(L)], where L is an anthracene-based ligand. Studies show that it induces cell death via inhibition of DNA synthesis. Moreover, because the complex is fluorescent, its uptake in cells was studied, and relative to the free anthracene-based ligand, uptake of the complex is accelerated and accumulation of the complex in the cell nucleus is observed.

Url:

https://api.istex.fr/ark:/67375/TPS-KGHJRWJM-D/fulltext.pdf

DOI: 10.1021/jm070039f

Affiliations:

Italie, Suisse

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Le document en format XML

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<front><div type="abstract">Organometallic ruthenium(II) complexes of the general formula [Ru(η6-p-cymene)Cl2(L)] and [Ru(η6-p-cymene)Cl(L)2][BPh4] with modified phenoxazine- and anthracene-based multidrug resistance (MDR) modulator ligands (L) have been synthesized, spectroscopically characterized, and evaluated in vitro for their cytotoxic and MDR reverting properties in comparison with the free ligands. For an anthracene-based ligand, coordination to a ruthenium(II) arene fragment led to significant improvement of cytotoxicity as well as Pgp inhibition activity. A similar, but weaker effect was also observed when using a benzimidazole-phenoxazine derivative as Pgp inhibitor. The most active compound in terms of both Pgp inhibition and cytotoxicity is [Ru(η6-p-cymene)Cl2(L)], where L is an anthracene-based ligand. Studies show that it induces cell death via inhibition of DNA synthesis. Moreover, because the complex is fluorescent, its uptake in cells was studied, and relative to the free anthracene-based ligand, uptake of the complex is accelerated and accumulation of the complex in the cell nucleus is observed.</div>
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Development of Ruthenium Antitumor Drugs that Overcome Multidrug Resistance Mechanisms

Development of Ruthenium Antitumor Drugs that Overcome Multidrug Resistance Mechanisms

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Abstract

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