Department of Chemistry, University of Exeter, Stocker Road, Exeter EX4 4QD, UK.
Bioorg Med Chem. 2013 Jun 1;21(11):2999-3009. doi: 10.1016/j.bmc.2013.03.071. Epub 2013 Apr 6.
A series of heterocyclic quinones based on benzofuran, benzothiophene, indazole and benzisoxazole has been synthesized, and evaluated for their ability to function as substrates for recombinant human NAD(P)H:quinone oxidoreductase (NQO1), a two-electron reductase upregulated in tumor cells. Overall, the quinones are excellent substrates for NQO1, approaching the reduction rates observed for menadione.
已经合成了一系列基于苯并呋喃、苯并噻吩、吲唑和苯并异恶唑的杂环醌,并评估了它们作为重组人 NAD(P)H:醌氧化还原酶 (NQO1) 的底物的能力,NQO1 是一种在肿瘤细胞中上调的双电子还原酶。总的来说,这些醌是 NQO1 的极好底物,接近观察到的亚甲二氢醌的还原速率。