<abstract xmlns="http://www.w3.org/1999/xhtml">Six gold(III) complexes with esters of cyclohexyl-functionalized ethylenediamine-<italic>N,N</italic>’-diacetate, general formula [AuCl2{(<italic>S,S</italic>)-R2eddch}]PF6, [(<italic>S,S</italic>)-eddch = (<italic>S,S</italic>)-ethylenediamine-<italic>N,N’</italic>-di-2-(3-cyclohexyl)propanoate, R = Me, Et, <italic>n</italic>-Pr, <italic>n</italic>-Bu, <italic>i</italic>-Bu, <italic>i</italic>-Am, <bold>1</bold>–<bold>6</bold>, respectively], were tested against cancer cell lines such as human melanoma Fem-x, human colon carcinoma LS174T and non-small cell lung carcinoma A549 as well as a non-cancerous human embryonic lung fibroblasts MRC-5 using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay with the aim of assessing <italic>in vitro</italic> antitumoral activity and selectivity. All investigated complexes showed lower cytotoxicity and better or similar selectivity in comparison to cisplatin, used as reference compound. Complex [AuCl2{(<italic>S,S</italic>)-(<italic>i</italic>-Am)2eddch}]PF6 (<bold>6</bold>) demonstrated the highest activity against Fem-x (IC50 = 14.98 ± 0.34 μM). Additionally, the same complex expressed 4.5 times higher selectivity than cisplatin.</abstract>

Six gold(III) complexes with esters of cyclohexyl-functionalized ethylenediamine-N,N’-diacetate, general formula [AuCl2{(S,S)-R2eddch}]PF6, [(S,S)-eddch = (S,S)-ethylenediamine-N,N’-di-2-(3-cyclohexyl)propanoate, R = Me, Et, n-Pr, n-Bu, i-Bu, i-Am, 1–6, respectively], were tested against cancer cell lines such as human melanoma Fem-x, human colon carcinoma LS174T and non-small cell lung carcinoma A549 as well as a non-cancerous human embryonic lung fibroblasts MRC-5 using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay with the aim of assessing in vitro antitumoral activity and selectivity. All investigated complexes showed lower cytotoxicity and better or similar selectivity in comparison to cisplatin, used as reference compound. Complex [AuCl2{(S,S)-(i-Am)2eddch}]PF6 (6) demonstrated the highest activity against Fem-x (IC50 = 14.98 ± 0.34 μM). Additionally, the same complex expressed 4.5 times higher selectivity than cisplatin.

Antiproliferative Activity of Gold(III) Complexes with Esters of Cyclohexyl-Functionalized Ethylenediamine-N,N’-Diacetate

Department of Chemistry and Biochemistry, Faculty of Agriculture

Department of Chemistry, Institute of Chemistry, Technology and Metallurgy

Department of Bioorganic Chemistry, Leibniz-Institute of Plant Biochemistry

Experimental and Applied Biomedical Research (EABR)

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Six gold(III) complexes with esters of cyclohexyl-functionalized ethylenediamine-N,N’-diacetate, general formula [AuCl2{(S,S)-R2eddch}]PF6, [(S,S)-eddch =...

Antiproliferative Activity of Gold(III) Complexes with Esters of Cyclohexyl-Functionalized Ethylenediamine-N,N’-Diacetate

Publicado en línea: 29 dic 2017

Páginas: 289 - 294

Recibido: 03 sept 2017

Aceptado: 30 sept 2017

DOI: https://doi.org/10.1515/sjecr-2017-0067

Palabras clave
cytotoxicity, gold(III) complexes, Redda type-ligands, selectivity

© 2017 Nebojša Pantelić et al., published by De Gruyter Open

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Antiproliferative Activity of Gold(III) Complexes with Esters of Cyclohexyl-Functionalized Ethylenediamine-N,N’-Diacetate

Publicado en línea: 29 dic 2017

Páginas: 289 - 294

Recibido: 03 sept 2017

Aceptado: 30 sept 2017

DOI: https://doi.org/10.1515/sjecr-2017-0067

Palabras clavecytotoxicity, gold(III) complexes, Redda type-ligands, selectivity

© 2017 Nebojša Pantelić et al., published by De Gruyter Open

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Palabras clave
cytotoxicity, gold(III) complexes, Redda type-ligands, selectivity