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Synthesis and characterisation of a novel tubulin-directed DO3A-colchicine conjugate with potential theranostic features |
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| Authors: | Wardle Nicholas J Kalber Tammy Bell Jimmy D Bligh S W Annie |
| Institution: | a Institute for Health and Research Policy, London Metropolitan University, Holloway Road, London N7 8DB, UK b Metabolic and Molecular Imaging Group, Imaging Sciences Department, MRC Clinical Sciences Centre, Imperial College London, Hammersmith Hospital, London W12 0NN, UK |
| Abstract: | Colchicine is a known tubulin binding agent enabling necrosis in tumors. A novel tubulin-directed DO3A-colchicine conjugate and its Gd(III) complex were prepared from N-deacetylcolchicine, coupling alkaloid and polyaza-alicyclic functions via a peptide coupling methodology. The longitudinal proton relaxivity of the Gd(III) complex in water at 4.7 T is 2.86 mM−1 s−1 and a similar efficacy as colchicine towards ovarian carcinoma cells in vitro. |
| Keywords: | Magnetic resonance imaging Contrast agent Gadolinium Colchicine Tubulin |
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