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 [AuCl 2 {(S,S)-R 2 eddch}]PF 6 , [(S,S)-eddch = (S,S)-ethylenediamine-N,N'-di-2-(3-cyclohexyl)propanoate, R = Me, Et,[1][2][3][4][5][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 [3][4] SAŽETAK Šest kompleksa zlata(III) sa cikloheksil-funkcionalizovanim estrima etilendiamin-N,N'-diacetata, opšte formule [AuCl 2 {(S,S)-R 2 eddch}]PF 6 , ((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 ćeli-jama MRC-5 (fetalni plućni fi broblast) korišćenjem

Recent development of gold(i) and gold(iii) complexes as therapeutic agents for cancer diseases

“…160 Dominelli et al synthesized the syn/antiisomers of dinuclear gold(I)-NHC complexes of the type Au 2 ( R L OH ) (PF 6 ) 2 (R = mesityl) containing 2-hydroxyethane-1,1-diyl-bridged bisimidazolylidene ligands 218-219. The complex syn Au 2 ( Mes L OH ) (PF 6 ) 2 (218) showed a higher selectivity against the MCF-7 cell line compared to cisplatin and significant antiproliferative activity with an IC 50 value of 1.22 AE 0.7 mM. 161 Jakob et al synthesized and characterized mono and disubstituted anthroyl ester bridgefunctionalized dinuclear gold(I) bis-NHC complexes.…”

“…All the complexes showed moderate antitumor activity with IC 50 values of about 20 μM. 218 Casado-Sánchez et al synthesized a new gold( iii ) complex with quinoline ligand, and evaluated the antiproliferative activity of the synthesized gold( iii ) complexes in six different human tumor cell lines by SRB analysis. The tolylsulfonamido complex 289 was found to be the most stable complex in DMSO and saline solution.…”