Bioorganic Chemistry 2010-02-01

Derivatives of thiocolchicine and its applications to CEM cells treatment using 19F magnetic resonance ex vivo.

Dorota Bartusik, Boguslaw Tomanek, Erika Lattová, Hélène Perreault, Jack Tuszynski, Gino Fallone

Index: Bioorg. Chem. 38(1) , 1-6, (2010)

Full Text: HTML

Abstract

It was shown, that cultured ex vivo human T-Lymphoblastoid (CEM) cells respond to synthesized thiocolchicine and fluorine thiocolchicine derivatives. The preparation of derivatives with substitution at C-3 and C-7 is described. All compounds were used at concentration from 1 nM to 1000 nM. Inhibitory effects of these compounds were examined in the three-dimensional (3-D) culture and cells morphology during treatment was monitored using 9.4 T MRI system. We performed studies of these compounds in CEM cells ex vivo using 1H and 19F Magnetic Resonance Imaging (MRI), 19F Magnetic Resonance Spectroscopy (MRS), High Performance Liquid Chromatography coupled with Ultra Violet (HPLC-UV) and Electron Impact Mass Spectrometry (EIMS). The results of the multi-technique approach are consistent with the fact that the new derivatives are more efficient than colchicine and thiocolchicine ex vivo.Crown Copyright 2009. Published by Elsevier Inc. All rights reserved.