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拉乌西坦酰胺 A 的全合成,一种索莫菌素酰胺 A 的单体同系物。

Total Synthesis of Laucysteinamide A, a Monomeric Congener of Somocystinamide A.

机构信息

Department of Chemistry and Forensic Science, Waynesburg University, 51 W College Street, Waynesburg, Pennsylvania 15370, United States.

Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography and Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, California 92093, United States.

出版信息

J Nat Prod. 2021 Mar 26;84(3):865-870. doi: 10.1021/acs.jnatprod.0c01317. Epub 2021 Feb 26.

Abstract

Laucysteinamide A () is a marine natural product isolated from the cyanobacterium and contains structural motifs found in promising cancer drug leads. The first total synthesis of and its analogues was achieved, which also enabled a concise formal synthesis of somocystinamide A (), a dimeric congener of that previously showed extremely potent antiproliferative activities. This work provides further insights on structure-activity relationships in this class of natural products.

摘要

拉西坦酰胺 A () 是一种从蓝藻中分离得到的海洋天然产物,其结构母核存在于有前景的抗癌药物先导化合物中。本文首次完成了 及其类似物的全合成,同时也实现了 somocystinamide A () 的简洁形式合成,后者是 的二聚体类似物,具有很强的抗增殖活性。该研究进一步揭示了此类天然产物的结构-活性关系。

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