期刊
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
卷 2018, 期 42, 页码 5830-5835出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.201800262
关键词
Total synthesis; Natural products; Cycloaddition; Asymmetric synthesis; Chiral auxiliaries; Biological activity
资金
- Bright Spark Unit, University of Malaya, Malaysia
- French Embassy in Malaysia
- Agence Nationale de la Recherche [CEBA: ANR-10-LABX-25-01]
Based on a bioinspired asymmetric Diels-Alder cycloaddition using a chiral Evans oxazolidinone, the first total synthesis of both enantiomers of two myrcene-derived cyclohexenyl chalcones, fislatifolione and fislatifolic acid, has been carried out. This strategy was also applied to the total synthesis of nicolaiodesin C. These natural products, as well as their synthetic intermediates, were evaluated by in-vitro affinity displacement assays, based on the modulation of Bcl-xL/Bak, Mcl-1/Bid, and Bcl-2-Bim interactions. This study showed that (+)-fislatifolic acid acts as a dual Bcl-xL/Mcl-1 inhibitor with micromolar activity, and that a Weinreb amide intermediate acts as an excellent Mcl-1/Bcl-2 dual inhibitor at the submicromolar level.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据