Silver derivatives of multi-donor heterocyclic thioamides as antimicrobial/anticancer agents: unusual bio-activity against methicillin resistant S. aureus, S. epidermidis, and E. faecalis and human bone cancer MG63 cell line

多供体杂环硫酰胺的银衍生物作为抗菌/抗癌剂:对耐甲氧西林金黄色葡萄球菌、表皮葡萄球菌、粪肠球菌和人类骨癌 MG63 细胞系具有不寻常的生物活性

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作者:Jaspreet K Aulakh, Tarlok S Lobana, Henna Sood, Daljit S Arora, Raminderjit Kaur, Jatinder Singh, Isabel Garcia-Santos, Manpreet Kaur, Jerry P Jasinski

Abstract

The basic aim of this study pertains to the synthesis of silver nitrate complexes and the study of their antimicrobial and anticancer bio-activity. A series of new silver(i) derivatives of N-substituted-imidazolidine-2-thiones (L-NR, R = Et, Pr n , Bu n , Ph), purine-6-thione (purSH2), 2-thiouracil (tucH2), pyrimidine-2-thione (pymSH) and pyridine-2-thione (pySH) of composition [Ag(S-L-NR)(PPh3)2(ONO2)] {R = Et (1), Pr n (2), Bu n (3), Ph (4)}, [Ag2(N,S-purSH2)2(μ-dppm)2](NO3)2·2H2O (5) (dppm = Ph2P-CH2-PPh2), [Ag(L)(PPh3)2](NO3) {L = N,S-purSH2 (6); S-tucH2 (7)}, [Ag(N,S-pymS)(PPh3)2](CH3OH) (8), and [Ag(N,S-pyS)(PPh3)2] (9) have been synthesized and structurally characterized. These new and some previously reported complexes {[Ag2(L-NH)4(PPh3)2](NO3)2 (10), [Ag(L-NMe)2(PPh3)](NO3) (11), and [Ag(S-bzimSH)2(PPh3)2](OAc) (12), L-NH = 1,3-imidazolidine-2-thione; L-NMe = 1-methyl-3-imidazolidine-2-thione and bzimSH2 = benzimidazoline-2-thione)} have shown moderate to high anti-microbial activity against Gram positive bacteria, namely methicillin resistant Staphylococcus aureus (MRSA) and Staphylococcus aureus (MTCC 740), and Gram negative bacteria, namely Staphylococcus epidermidis (MTCC 435), Enterococcus faecalis (MTCC 439), Shigella flexneri (MTCC 1457) and a yeast Candida albicans (MTCC 22). These complexes have also been found to be bio-safe as studied using MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide] assay. The anti-tumor study of silver complexes against human osteosarcoma cell line (MG63) has shown IC50 values in the range of 6-33 μM.

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