Antiplasmodial activities of gold(I) complexes involving functionalized N-heterocyclic carbenes
Identifieur interne : 000124 ( France/Analysis ); précédent : 000123; suivant : 000125Antiplasmodial activities of gold(I) complexes involving functionalized N-heterocyclic carbenes
Auteurs : Catherine Hemmert [France] ; Arba Pramundita Ramadani [France] ; Luca Boselli [France] ; Alvaro Fernandez Alvarez [France] ; Lucie Paloque [France] ; Jean-Michel Augereau [France] ; H. Gornitzka [France] ; F. Benoit-Vical [France]Source :
- Bioorganic and Medicinal Chemistry [ 0968-0896 ] ; 2016.
Abstract
A series of twenty five molecules, including imidazolium salts functionalized by N-, O- or S-containing groups and their corresponding cationic, neutral or anionic gold(I) complexes were evaluated on Plasmodium falciparum in vitro and then on Vero cells to determine their selectivity. Among them, eight new compounds were synthesized and fully characterized by spectroscopic methods. The X-ray structures of three gold(I) complexes are presented. Except one complex (18), all the cationic gold(I) complexes show potent antiplasmodial activity with IC50 in the micro-and submicromolar range, correlated with their lipophilicity. Structure-activity relationships enable to evidence a lead-complex (21) displaying a good activity (IC50 = 210 nM) close to the value obtained with chloroquine (IC50 = 514 nM) and a weak cytotoxicity. (C) 2016 Elsevier Ltd. All rights reserved.
Url:
DOI: 10.1016/j.bmc.2016.05.023
Affiliations:
Links toward previous steps (curation, corpus...)
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Hal:hal-01937596Le document en format XML
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<author><name sortKey="Fernandez Alvarez, Alvaro" sort="Fernandez Alvarez, Alvaro" uniqKey="Fernandez Alvarez A" first="Alvaro" last="Fernandez Alvarez">Alvaro Fernandez Alvarez</name>
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<idno type="DOI">10.1016/j.bmc.2016.05.023</idno>
<series><title level="j">Bioorganic and Medicinal Chemistry</title>
<idno type="ISSN">0968-0896</idno>
<imprint><date type="datePub">2016</date>
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<front><div type="abstract" xml:lang="en"> <p>A series of twenty five molecules, including imidazolium salts functionalized by N-, O- or S-containing groups and their corresponding cationic, neutral or anionic gold(I) complexes were evaluated on Plasmodium falciparum in vitro and then on Vero cells to determine their selectivity. Among them, eight new compounds were synthesized and fully characterized by spectroscopic methods. The X-ray structures of three gold(I) complexes are presented. Except one complex (18), all the cationic gold(I) complexes show potent antiplasmodial activity with IC50 in the micro-and submicromolar range, correlated with their lipophilicity. Structure-activity relationships enable to evidence a lead-complex (21) displaying a good activity (IC50 = 210 nM) close to the value obtained with chloroquine (IC50 = 514 nM) and a weak cytotoxicity. (C) 2016 Elsevier Ltd. All rights reserved.</p>
</div>
</front>
</TEI>
<affiliations><list><country><li>France</li>
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<tree><country name="France"><noRegion><name sortKey="Hemmert, Catherine" sort="Hemmert, Catherine" uniqKey="Hemmert C" first="Catherine" last="Hemmert">Catherine Hemmert</name>
</noRegion>
<name sortKey="Augereau, Jean Michel" sort="Augereau, Jean Michel" uniqKey="Augereau J" first="Jean-Michel" last="Augereau">Jean-Michel Augereau</name>
<name sortKey="Benoit Vical, F" sort="Benoit Vical, F" uniqKey="Benoit Vical F" first="F." last="Benoit-Vical">F. Benoit-Vical</name>
<name sortKey="Boselli, Luca" sort="Boselli, Luca" uniqKey="Boselli L" first="Luca" last="Boselli">Luca Boselli</name>
<name sortKey="Fernandez Alvarez, Alvaro" sort="Fernandez Alvarez, Alvaro" uniqKey="Fernandez Alvarez A" first="Alvaro" last="Fernandez Alvarez">Alvaro Fernandez Alvarez</name>
<name sortKey="Gornitzka, H" sort="Gornitzka, H" uniqKey="Gornitzka H" first="H." last="Gornitzka">H. Gornitzka</name>
<name sortKey="Paloque, Lucie" sort="Paloque, Lucie" uniqKey="Paloque L" first="Lucie" last="Paloque">Lucie Paloque</name>
<name sortKey="Ramadani, Arba Pramundita" sort="Ramadani, Arba Pramundita" uniqKey="Ramadani A" first="Arba Pramundita" last="Ramadani">Arba Pramundita Ramadani</name>
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