Abstract
This paper describes synthesis, characterization (NMR, FT-IR, microanalysis, and X-ray crystallography),in vitroanticancer activity ofortho/para-xylyl linked bis-imidazolium salts (4-5) and respective dinuclear Ag(I)N-heterocyclic carbene (NHC) complexes (6-7). All the compounds were tested for their cytotoxicity against human colorectal cancer (HCT 116) and breast cancer (MCF-7) cell lines. According to cell viability measurements using MTT assay, all the complexes (6-7) showed a dose-dependent cytotoxic activity against both the cell lines, whereas respective salts (4-5) proved to be inactive. The complexes (6-7) demonstrated significant activity with IC50values range 5.6–20.3 μM for HCT 116 and 1.12–6.38 μM for MCF-7. 5-Fluorouracil was used as standard drug (IC50= 5.9 μM) for HCT 116, whereas tamoxifen was used as standard drug for MCF-7 (IC50= 14 μM) cell line.
Highlights
New drugs to fight cancer are constantly needed
The percentage of growth inhibition was calculated from the optical density (OD) obtained from MTT assay. 5-FU and tamoxifen were used as the standard reference drugs for HCT 116 and MCF-7 cells, respectively
The use of acetonitrile or 1,4-dioxane as a reaction medium for the synthesis of xylyl linked bis-azolium salts is highly recommended because by using either of the solvents, bis-azolium salts can be collected either directly as a solid from reaction medium using common filtration method or by decantation of reaction medium when the product settles as a thick yellowish fluid at the bottom of the flask (Scheme 1) [49]
Summary
New drugs to fight cancer are constantly needed. Every year, more than 10 million new cases of cancer are registered around the globe and more than half of the patients die [1]. Today a number of platinum based drugs (oxaliplatin, carboplatin, nedaplatin, and lobaplatin) are serving the cancer patients worldwide [3, 11]. The biological importance of azole derivatives is due to their structural resemblance to the naturally occurring nucleotides, which allows them to interact with the biopolymers of the living system [32]. Coupling of these biologically compatible moieties generates a pharmaceutically enhanced class of compounds known as Ag(I)-NHC complexes. The current work is an effort to further explore this area of research
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
