Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2018 Jul 31;47(30):10035-10045.
doi: 10.1039/c8dt01778f.

Synthesis, in vitro cytotoxicity, and structure-activity relationships (SAR) of multidentate oxidovanadium(iv) complexes as anticancer agents

Affiliations

Synthesis, in vitro cytotoxicity, and structure-activity relationships (SAR) of multidentate oxidovanadium(iv) complexes as anticancer agents

Lubin Ni et al. Dalton Trans. .

Abstract

Multidentate oxidovanadium(iv) complexes with different geometric configurations [VO(ox)(bpy)(H2O)] 1, [VO(ox)(phen)(H2O)] 2, [VO(ida)(bpy)]·2H2O 3, (phen)[VO(ida)(phen)]·4H2O 4, and (Hphen)[VO(H2O)(nta)]·2H2O 5 [ox = oxalic acid, bpy = 2,2'-bipyridine, phen = 1,10-phenanthroline, ida = iminodiacetic acid, nta = nitrilotriacetic acid] have been obtained from the reactions of oxidovanadium sulfate or vanadium pentoxide with oxalates, amino-polycarboxylates and N-heterocyclic ligands in neutral solution by the hydrothermal method, and have been fully characterized by elemental, thermogravimetric analyses and single crystal X-ray diffraction, as well as a wide range of spectroscopic techniques such as FT-IR, UV/Vis, NMR, ESI-MS. The anti-tumor properties of oxidovanadium compounds 1-5 were further evaluated in human HepG2 and SMMC-7721 hepatocellular carcinoma cell lines in vitro. The profiles of cytotoxicity, cell cycle distribution, as well as cell apoptosis upon test compound exposure, were determined by MTT and flow cytometry assays. Compound 2 exhibited a much higher anti-tumor activity than others. The IC50 values of 2 were 5.34 ± 0.034 μM and 29.07 ± 0.017 μM in SMMC-7721 and HepG2 cells after 48 h treatment, respectively. Furthermore, compound 2 could significantly arrest the cell cycle in the S and G2/M phases and further induce cell apoptosis in a dose-dependent manner. The structure-activity relationship (SAR) studies revealed that structural elements, for example, metal components, variations of coordination mode, labile water molecules, chelated ligands etc., probably exert an essential cooperative effect on the antitumor activity. In short, these findings not only provide an accessible model system to exploit V-based complexes as potential simple, safe and effective multifunctional antitumor agents, but also open up a rational approach to shed new light on the selection and optimization of ideal drug candidates.

PubMed Disclaimer

MeSH terms

LinkOut - more resources