title: Synthesis and characterisation of a novel tubulin-directed DO3A-colchicine conjugate with potential theranostic features.
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.
authors.affiliation: Institute for Health and Research Policy, London Metropolitan University, Holloway Road, London N7 8DB, UK.
authors.forename: Nicholas J
authors.initials: NJ
authors.lastname: Wardle
authors.forename: Tammy
authors.initials: T
authors.lastname: Kalber
authors.forename: Jimmy D
authors.initials: JD
authors.lastname: Bell
authors.forename: S W Annie
authors.initials: SW
authors.lastname: Bligh
mesh_terms: D045744:Cell Line, Tumor; D003078:Colchicine / Q000737:chemistry / Q000378:metabolism; D005260:Female; D006801:Humans; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D010051:Ovarian Neoplasms / Q000503:physiopathology; D014404:Tubulin / Q000378:metabolism
chemical_list: C469806:Gd(III)-DO3A complex; D009942:Organometallic Compounds; D014404:Tubulin; D003078:Colchicine