Department of Organic Chemistry, University of Santiago de Compostela, Campus Vida, 15782 Santiago de Compostela, Spain.
Org Biomol Chem. 2013 Jan 21;11(3):515-22. doi: 10.1039/c2ob27127c. Epub 2012 Dec 3.
Access to some 7,9-dideoxy analogues of pancratistatin was achieved by combining our previously reported nitroenal/dioxanone annulation (to form ring C) with a hetero-Diels-Alder/aromatization path to build the dihydroisoquinolinone subunit (rings A and B); testing of their antiproliferative activity afforded some clues about the role of aromatic substituents in pancratistatin's pharmacophore.
通过结合我们之前报道的硝基亚胺/二氧杂环戊酮环化(形成环 C)以及杂[4+2]环加成/芳构化路径,获得了一些 7,9-二脱氧类似物的访问权限潘克拉他汀; 对其抗增殖活性的测试提供了有关芳香取代基在潘克拉他汀药效团中的作用的一些线索。