aspergiolides A 和 B：核心结构的建立和结构类似物的合成。
Aspergiolides A and B: Core Structural Establishment and Synthesis of Structural Analogues.
机构信息
Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy , Ocean University of China , Qingdao 266003 , P.R. China.
Laboratory for Marine Drugs and Bioproducts of Qingdao National Laboratory for Marine Science and Technology , Qingdao 266237 , P.R. China.
出版信息
J Org Chem. 2019 Apr 5;84(7):4451-4457. doi: 10.1021/acs.joc.8b03185. Epub 2019 Mar 21.
The core structure of marine natural products aspergiolides A (1a) and B (1b) was achieved via a concise, two-step procedure with satisfactory yield. Based on this protocol, a natural products mimic library containing 25 structural simplified analogues of 1a was then constructed. Several prepared analogues showed potential cytotoxic activity against five different tumor cell lines, and compound 7bb, in particular, exhibited cytotoxicity comparable to that of 1a.
海洋天然产物 aspergiolides A（1a）和 B（1b）的核心结构通过简洁的两步法以令人满意的产率得到实现。基于该方案，随后构建了包含 25 个 1a 结构简化类似物的天然产物模拟物库。几种制备的类似物显示出对五种不同肿瘤细胞系的潜在细胞毒性活性，特别是化合物 7bb 表现出与 1a 相当的细胞毒性。
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