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

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1770-3. doi: 10.1016/j.bmcl.2011.12.071. Epub 2011 Dec 21.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimalarials* / chemical synthesis
  • Antimalarials* / chemistry
  • Antimalarials* / pharmacology
  • Humans
  • Indoles / chemical synthesis
  • Indoles / chemistry*
  • Indoles / pharmacology
  • Isoquinolines / chemical synthesis*
  • Isoquinolines / chemistry
  • Isoquinolines / pharmacology*
  • Molecular Structure
  • Plasmodium falciparum / drug effects*
  • Small Molecule Libraries
  • Structure-Activity Relationship

Substances

  • Antimalarials
  • Indoles
  • Isoquinolines
  • Small Molecule Libraries
  • dihydrousambarensine