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- Title
Synthesis, Molecular Docking and Cytotoxic Activity Evaluation of Organometallic Thiolated Gold(I) Complexes.
- Authors
Faghih, Zeinab; Kachoei, Alireza Yazdani; Alizadeh, Hossein; Emamdoost, Suphia; Shirkhan, Shima; Fereidoonnezhad, Masood
- Abstract
The complex [(PhCH2NC)AuCl], 1, was prepared by the reaction of [(Me2S)AuCl], A, with an equimolar amount of benzyl isocyanide (PhCH2NC) ligand. Through a salt metathesis reaction, the chloride ligand in 1 was replaced by potassium benzothiazole-2-thiolate (Kbt) and potassium benzoimidazole-2-thiolate (Kbi) to afford complexes (PhCH2NC)Au(κ¹-S-bt)], 2a and (PhCH2NC)Au(κ¹-S-bi)], 2b, respectively, which were characterized by NMR spectroscopy. The cytotoxic activities of 2a and 2b were evaluated against three human cancer cell lines, including A549 (lung), SKOV3 (ovary), and MCF-7 (breast). Our results indicated that 2a exhibited comparable cytotoxicity on investigated cell lines with cisplatin. It showed a good antiproliferative activity with IC50 of 19.46, 11.76 and 13.27 μM against A549, SKOV3 and MCF-7 cell lines, respectively. The effects of these complexes on the proliferation of the non-tumorigenic epithelial breast cell line (MCF-10A) showed their good selectivity between the tumorigenic and non-tumorigenic cell lines. Molecular docking simulation studies were also conducted to determine the specific binding site and binding mode of the synthesized gold complexes to DNA and thioredoxinreductase (TrxR) as their proposed targets.
- Subjects
MOLECULAR docking; CELL lines; BINDING sites; NUCLEAR magnetic resonance spectroscopy; METATHESIS reactions
- Publication
Iranian Journal of Pharmaceutical Research, 2020, Vol 19, Issue 3, p134
- ISSN
1735-0328
- Publication type
Article
- DOI
10.22037/ijpr.2020.1101118