کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369320 | 981772 | 2014 | 6 صفحه PDF | دانلود رایگان |
131Iodine-labelled (meta-iodobenzyl)guanidine ([131I]-mIBG) and busulfan [butane-1,4-diylbis(methanesulfonate)] are well-established pharmaceuticals in neuroblastoma therapy. We report the design, synthesis, and testing of hybrid molecules—mBBG and pBBG—which combine key structural features of (meta-iodobenzyl)guanidine and busulfan: they contain a benzylguanidine moiety for accumulating in neuroblastoma cells via the noradrenaline transporter and, in the meta- or para-position, respectively, one of the two identical alkylating motives of busulfan for killing cells. Uptake and toxicity of hybrids mBBG and pBBG in human neuroblastoma cells compared favorably to their ancestors [131I]-mIBG and busulfan.
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Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 12, 15 June 2014, Pages 2728–2733