作者:Veselin Nasufović、Florian Küllmer、Johanna Bößneck、Hans‐Martin Dahse、Helmar Görls、Peter Bellstedt、Pierre Stallforth、Hans‐Dieter Arndt
DOI:10.1002/chem.202100989
日期:2021.8.11
The first total synthesis of the actin-stabilizing marine natural product geodiamolide H was achieved. Solid-phase based peptide assembly paired with scalable stereoselective syntheses of polyketide building blocks and an optimized esterification set the stage for investigating the key ring-closing metathesis. Geodiamolide H and synthetic analogues were characterized for their toxicity and for antiproliferative
首次实现了肌动蛋白稳定海洋天然产物 Geodiamolide H 的全合成。基于固相的肽组装与聚酮化合物结构单元的可扩展立体选择性合成以及优化的酯化相结合,为研究关键的闭环复分解奠定了基础。Geodiamolide H 和合成类似物的毒性和抗细胞增殖作用得到了表征,通过表征体外肌动蛋白聚合诱导,并通过计算机对接 F-肌动蛋白靶点和属性计算,以更好地理解结构-活性关系。特别行政区)。geodiamolide H 的非天然类似物被发现是该系列中最有效的,这表明工具化合物设计具有巨大的潜力。