Synthesis and characterisation of a novel tubulin-directed DO3A–colchicine conjugate with potential theranostic features
Author(s)
Author(s)
Wardle, N. J.
Kalber, T.
Bell, J. D.
Date Issued
2011
Publisher
Elsevier
Journal
Bioorganic & Medicinal Chemistry Letters
Volume
21
Issue
11
Start page
3346
End page
3348
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.
SFU Affiliated Publication
No
Availability at SFU Library
No database links found.