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.
Copyright © 2012 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antimalarials* / chemical synthesis
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Antimalarials* / chemistry
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Antimalarials* / pharmacology
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Humans
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Indoles / chemical synthesis
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Indoles / chemistry*
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Indoles / pharmacology
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Isoquinolines / chemical synthesis*
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Isoquinolines / chemistry
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Isoquinolines / pharmacology*
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Molecular Structure
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Plasmodium falciparum / drug effects*
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Small Molecule Libraries
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Structure-Activity Relationship
Substances
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Antimalarials
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Indoles
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Isoquinolines
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Small Molecule Libraries
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dihydrousambarensine