Title | Synthesis and characterisation of a novel tubulin-directed DO3A–colchicine conjugate with potential theranostic features |
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Authors | Wardle, N.J., Kalber, T., Bell, J.D. and Bligh, S.W.A. |
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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. |
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Journal | Bioorganic and Medicinal Chemistry Letters |
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Journal citation | 21 (11), pp. 3346-3348 |
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ISSN | 0960-894X |
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Year | Jun 2011 |
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Publisher | Pergamon |
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Digital Object Identifier (DOI) | https://doi.org/10.1016/j.bmcl.2011.04.014 |
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Publication dates |
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Published | Jun 2011 |
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