کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5219698 | 1383365 | 2012 | 8 صفحه PDF | دانلود رایگان |
Semi-synthetic N-13 alkylated analogues of the cytotoxic marine alkaloid discorhabdin C have been found to exhibit cytotoxicity towards tumour cell lines at comparable levels to that of the natural product. Incorporation of an ethylenediamine linker facilitated the synthesis of a variety of fluorophore-labelled probes, of which dansyl analogue 20 exhibited biological activity, providing a tool for mechanism of action and cellular localization studies. An alternative probe design was also exemplified, whereby a bioactive alkyne-terminated analogue (24) was found to undergo Huisgen 1,3-dipolar cycloaddition ‘click’ reactions with fluorescent azides, enabling studies directed towards activity-based protein profiling.
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Journal: Tetrahedron - Volume 68, Issue 15, 15 April 2012, Pages 3187–3194