Antiproliferative activity of gold (III) complexes with esters of cyclohexyl-functionalized ethylenediamine-N,N'-diacetate

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 fi broblasts 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.

Šest kompleksa zlata(III) sa cikloheksil-funkcionalizovanim estrima etilendiamin-N,N'-diacetata, opšte formule [AuCl2{(S,S)-R2eddch}]PF6, ((S,S)-eddch = (S,S)-etilendiamin- N,N'-di-2-(3-cicloheksil)propanoat, R = Me, Et, n-Pr, n-Bu, i-Bu, i-Am, 1-6), ispitivano je na humanim ćelijskim linijama malignog melanoma Fem-x, karcinoma debelog creva LS174T, karcinoma pluća A549 kao i normalnim ćelijama MRC-5 (fetalni plućni fi broblast) korišćenjem 3-(4,5-dimetiltiazol- 2-yl)-2,5-difeniltetrazolium bromid (MTT) testa u cilju procene in vitro antitumorske aktivnosti i selektivnosti. Svi ispitivani kompleksi pokazali su manju citotoksičnost i bolju ili sličnu selektivnost u odnosu na cisplatinu koja je korišćena kao referentna supstanca. Kompleks 6 je pokazao najveću aktivnost sa IC50 (Fem-x) vrednošću od 14,98 ± 0,34 μM. Takođe, isti kompleks pokazuje 4,5 puta veću selektivnost od cisplatine.