Imperial College London

Prof. Ramon Vilar

Faculty of Natural SciencesDepartment of Chemistry

Professor of Medicinal Inorganic Chemistry
 
 
 
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Contact

 

+44 (0)20 7594 1967r.vilar Website

 
 
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Location

 

301HMolecular Sciences Research HubWhite City Campus

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Summary

 

Publications

Citation

BibTex format

@article{Vilar:2016:10.1039/C5DT04753F,
author = {Vilar, Compte R and Collins, J and Woscholski, R and Cilibrizzi, A and Leatherbarrow, RJ and Fedorova, M and Whyte, G and Guterman, I and Mak, LH},
doi = {10.1039/C5DT04753F},
journal = {Dalton Transactions},
pages = {7104--7113},
title = {Vanadyl complexes with dansyl-labelled di-picolinic acid ligands: synthesis, phosphatase inhibition activity and cellular uptake studies},
url = {http://dx.doi.org/10.1039/C5DT04753F},
volume = {45},
year = {2016}
}

RIS format (EndNote, RefMan)

TY  - JOUR
AB - Vanadium complexes have been previously utilised as potent inhibitors of cysteine based phosphatases (CBPs) . Herein, we present the synthesis and characterisation of two new fluorescently labelled vanadyl complexes (14 and 15 ) with bridged dipicolinic acid ligand. These compounds differ significantly from previous vanadyl complexes with phosphatase inhibition properties in that the metal-chelating part is a single tetradentate unit, which should afford greater stability and scope for synthetic elaboration then the earlier complexes. These new complexes inhibit a selection of cysteine based phosphatases (CBPs) in the nM range with some selectivity. Fluorescence spectroscopic studies (including fluorescence anisotropy) were carried out to demonstrate that the complexes are not simply acting as vanadyl delivery vehicles but they interact with the proteins. Finally, we present preliminary fluorescence microscopy studies to demonstrate that the complexes are cell permeable and localise throughout the cytoplasm of NIH3T3 cells.
AU - Vilar,Compte R
AU - Collins,J
AU - Woscholski,R
AU - Cilibrizzi,A
AU - Leatherbarrow,RJ
AU - Fedorova,M
AU - Whyte,G
AU - Guterman,I
AU - Mak,LH
DO - 10.1039/C5DT04753F
EP - 7113
PY - 2016///
SN - 1477-9226
SP - 7104
TI - Vanadyl complexes with dansyl-labelled di-picolinic acid ligands: synthesis, phosphatase inhibition activity and cellular uptake studies
T2 - Dalton Transactions
UR - http://dx.doi.org/10.1039/C5DT04753F
UR - http://hdl.handle.net/10044/1/30274
VL - 45
ER -