Synthesis and evaluation of a novel series of indoloisoquinolines as small molecule anti-malarial leads

A group of novel synthetic indoloisoquinolines was prepared and its potential as a novel series of smallmolecule 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. (C) 2012 Elsevier Ltd. All rights reserved.