School of Medicine, Keele University, UK.
Bioorg Med Chem Lett. 2012 Feb 15;22(4):1770-3. doi: 10.1016/j.bmcl.2011.12.071. Epub 2011 Dec 21.
A group of novel synthetic indoloisoquinolines was prepared and its potential as a novel series of small-molecule anti-malarial leads was assessed. The structure-activity relationship on variation of three distinct regions of chemical space was investigated. A lead compound was generated with an activity close to that observed for a known anti-malarial natural product, dihydrousambarensine, that shares the indoloisoquinoline template structure.
一组新型合成吲哚异喹啉被制备出来，并评估了其作为新型小分子抗疟先导物的潜力。研究了在三个不同化学空间区域变化时的构效关系。生成了一个具有与已知抗疟天然产物二氢桑巴伦辛（具有相同的吲哚异喹啉模板结构）相近活性的先导化合物。
