کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1324582 | 977346 | 2009 | 11 صفحه PDF | دانلود رایگان |

A new bifunctional carborane ligand was prepared as a platform for the development of targeted molecular radioimaging and therapy agents. The carborane derivative was synthesized bearing a glucose substituent to increase the water solubility of the ligand and a benzoic acid group as a site for linking to amine containing targeting vectors. A convenient method to conjugate the ligand and the non-glycosylated analogue to amino groups was developed using simple active esters which were combined with a model amine generating two new N,N-diethyl(aminoethyl) benzamide derivatives. These were labelled with 125I in good yield and the log P values measured for [125I]-15 (log P = 0.82 ± 0.04) and [125I]-16 (log P = 1.53 ± 0.01). The benzamides were also evaluated for their capacity to bind to B16F10 melanoma cells where the hydrophilic compound showed low binding while [125I]-16 showed modest uptake (30.7 ± 2.2%) after 24 h.
Two new bifunctional nido-carboraneligands were prepared and labelled with 125I. These compounds are platforms for preparing targeted molecular imaging and therapy agentsFigure optionsDownload as PowerPoint slide
Journal: Journal of Organometallic Chemistry - Volume 694, Issue 11, 1 May 2009, Pages 1736–1746