Front Cover: Helenalin Analogues Targeting NF‐κB p65: Thiol Reactivity and Cellular Potency Studies of Varied Electrophiles (ChemMedChem 4/2018),ChemMedChem

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Front Cover: Helenalin Analogues Targeting NF‐κB p65: Thiol Reactivity and Cellular Potency Studies of Varied Electrophiles (ChemMedChem 4/2018)
ChemMedChem ( IF 3.6 ) Pub Date : 2018-02-20 , DOI: 10.1002/cmdc.201800079
John C. Widen ₁ , Aaron M. Kempema ₁ , Jordan W. Baur ₁ , Hannah M. Skopec ₁ , Jacob T. Edwards ₁ , Tenley J. Brown ₁ , Dennis A. Brown ₁ , Frederick A. Meece ₁ , Daniel A. Harki ₁

Affiliation

The Front Cover shows two race cars, representing an endocyclic enone and an exocyclic methylene butyrolactone, racing to complete hetero‐Michael additions to a biological thiol. This work describes the synthesis of simplified helenalin analogues containing combinations of endocyclic enones and exocyclic methylene butyrolactones. Thiol reactivity kinetics and NF‐κB inhibitory activities of the simplified helenalin analogues is reported, which provides insights into the contributions of the individual electrophiles to biological potency. More information can be found in the Full Paper by Daniel A. Harki et al. on page 303 in Issue 4, 2018 (DOI: 10.1002/cmdc.201700752).

中文翻译：

封面：针对NF-κBp65的Helenalin类似物：各种亲电试剂的硫醇反应性和细胞效能研究（ChemMedChem 4/2018）

封面显示了两辆赛车，分别代表一个内环烯酮和一个环亚甲基丁内酯，它们竞相完成对生物硫醇的异-迈克尔加成反应。这项工作描述了简化的海兰肽类似物的合成，该类似物包含环内烯酮和环外亚甲基丁内酯的组合。报道了简化的海蓝素类似物的硫醇反应动力学和NF-κB抑制活性，这为了解各个亲电试剂对生物效能的贡献提供了见解。可以在Daniel A. Harki等人的论文全文中找到更多信息。就在第4期，2018第303页（：10.1002 / cmdc.201700752 DOI）。

更新日期：2018-02-20

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