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柔性核苷类似物——抗丝状病毒的新型疗法。

Flex-nucleoside analogues - Novel therapeutics against filoviruses.

作者信息

Yates Mary K, Raje Mithun R, Chatterjee Payel, Spiropoulou Christina F, Bavari Sina, Flint Mike, Soloveva Veronica, Seley-Radtke Katherine L

机构信息

Department of Chemistry and Biochemistry, University of Maryland Baltimore County, Baltimore, MD 21250, United States.

Viral Special Pathogens Branch, Centers for Disease Control and Prevention, Atlanta, GA 30329, United States.

出版信息

Bioorg Med Chem Lett. 2017 Jun 15;27(12):2800-2802. doi: 10.1016/j.bmcl.2017.04.069. Epub 2017 Apr 22.

DOI:10.1016/j.bmcl.2017.04.069
PMID:28465098
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5626011/
Abstract

Fleximers, a novel type of flexible nucleoside that have garnered attention due to their unprecedented activity against human coronaviruses, have now exhibited highly promising levels of activity against filoviruses. The Flex-nucleoside was the most potent against recombinant Ebola virus in Huh7 cells with an EC=2μM, while the McGuigan prodrug was most active against Sudan virus-infected HeLa cells with an EC of 7μM.

摘要

柔性核苷是一种新型的柔性核苷，因其对人类冠状病毒具有前所未有的活性而备受关注，现在已显示出对丝状病毒具有高度可观的活性水平。Flex-核苷在Huh7细胞中对重组埃博拉病毒的活性最强，其半数有效浓度（EC）为2μM，而麦奎根前药对苏丹病毒感染的HeLa细胞活性最高，其半数有效浓度为7μM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/991e/7125901/6b53dbc8d8b8/gr4_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/991e/7125901/079fc8b26b81/fx1_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/991e/7125901/e45ca473b74a/gr1_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/991e/7125901/6d875efb9a78/gr2_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/991e/7125901/bf8507784119/gr3_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/991e/7125901/6b53dbc8d8b8/gr4_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/991e/7125901/079fc8b26b81/fx1_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/991e/7125901/e45ca473b74a/gr1_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/991e/7125901/6d875efb9a78/gr2_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/991e/7125901/bf8507784119/gr3_lrg.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/991e/7125901/6b53dbc8d8b8/gr4_lrg.jpg

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