1610616-07-3Relevant academic research and scientific papers
Synthesis and biological effects of new hybrid compounds composed of benzylguanidines and the alkylating group of busulfan on neuroblastoma cells
Hampel, Thomas,Bruns, Marietta,Bayer, Melanie,Handgretinger, Rupert,Bruchelt, Gernot,Brückner, Reinhard
, p. 2728 - 2733 (2014)
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.
