缺氧驱动硫嘌呤从其硝苄基前药中消除。
Hypoxia-driven elimination of thiopurines from their nitrobenzyl prodrugs.
作者信息
Thomson Peter, Naylor Matthew A, Stratford Michael R L, Lewis Gemma, Hill Sally, Patel Kantilal B, Wardman Peter, Davis Peter D
机构信息
University of Oxford, Gray Cancer Institute, Mount Vernon Hospital, Northwood, Middlesex HA6 2JR, UK.
出版信息
Bioorg Med Chem Lett. 2007 Aug 1;17(15):4320-2. doi: 10.1016/j.bmcl.2007.05.018. Epub 2007 May 13.
A novel bioreductive prodrug of 6-thioguanine, 2-amino-6-[2-(4-nitrophenyl)prop-2-ylsulfanyl]-9H-purine, containing a gem-dimethyl thioether linkage, was synthesised and compared with its unsubstituted analogue. In A549 whole cell experiments hypoxia selective release of 6-thioguanine was observed with the substituted prodrug only.
合成了一种新型的6-硫鸟嘌呤生物还原前药，即2-氨基-6-[2-(4-硝基苯基)丙-2-基硫烷基]-9H-嘌呤，其含有偕二甲基硫醚键，并将其与其未取代的类似物进行了比较。在A549全细胞实验中，仅观察到取代前药在缺氧条件下选择性释放6-硫鸟嘌呤。
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