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苯并呋喃、苯并噻吩、吲唑和苯并异恶唑-醌：NAD(P)H：醌氧化还原酶 1 的优异底物。

Benzofuran-, benzothiophene-, indazole- and benzisoxazole-quinones: excellent substrates for NAD(P)H:quinone oxidoreductase 1.

机构信息

Department of Chemistry, University of Exeter, Stocker Road, Exeter EX4 4QD, UK.

出版信息

Bioorg Med Chem. 2013 Jun 1;21(11):2999-3009. doi: 10.1016/j.bmc.2013.03.071. Epub 2013 Apr 6.

DOI:10.1016/j.bmc.2013.03.071
PMID:23635904
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3697102/
Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/94e734099631/nihms474477f9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/19d51e258ff3/nihms474477f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/de55fce1ec3d/nihms474477f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/cbff5d6cde07/nihms474477f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/1fa9b82e8846/nihms474477f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/724755a07412/nihms474477f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/f1581f2752af/nihms474477f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/b72f7960af36/nihms474477f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/38b243d2cf87/nihms474477f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/94e734099631/nihms474477f9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/19d51e258ff3/nihms474477f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/de55fce1ec3d/nihms474477f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/cbff5d6cde07/nihms474477f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/1fa9b82e8846/nihms474477f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/724755a07412/nihms474477f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/f1581f2752af/nihms474477f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/b72f7960af36/nihms474477f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/38b243d2cf87/nihms474477f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/63f2/3697102/94e734099631/nihms474477f9.jpg

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