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Exploration of 3-methylisoquinoline-4-carbonitriles as protein kinase A inhibitors of Plasmodium falciparum.
Buskes, Melissa J; Harvey, Katherine L; Prinz, Boris; Crabb, Brendan S; Gilson, Paul R; Wilson, David J D; Abbott, Belinda M.
Afiliación
  • Buskes MJ; Department of Chemistry and Physics, La Trobe Institute for Molecular Science, La Trobe University, Melbourne, Victoria 3086, Australia.
  • Harvey KL; Centre for Biomedical Research, Burnet Institute, Melbourne, Victoria 3004, Australia.
  • Prinz B; Centre for Biomedical Research, Burnet Institute, Melbourne, Victoria 3004, Australia.
  • Crabb BS; Centre for Biomedical Research, Burnet Institute, Melbourne, Victoria 3004, Australia; Monash University, Melbourne, Victoria 3800, Australia; University of Melbourne, Melbourne 3010, Australia.
  • Gilson PR; Centre for Biomedical Research, Burnet Institute, Melbourne, Victoria 3004, Australia; Monash University, Melbourne, Victoria 3800, Australia.
  • Wilson DJ; Department of Chemistry and Physics, La Trobe Institute for Molecular Science, La Trobe University, Melbourne, Victoria 3086, Australia.
  • Abbott BM; Department of Chemistry and Physics, La Trobe Institute for Molecular Science, La Trobe University, Melbourne, Victoria 3086, Australia. Electronic address: b.abbott@latrobe.edu.au.
Bioorg Med Chem ; 24(11): 2389-96, 2016 06 01.
Article en En | MEDLINE | ID: mdl-27112453
A series of isoquinolines have been evaluated in a homology model of Plasmodium falciparum Protein Kinase A (PfPKA) using molecular dynamics. Synthesis of these compounds was then undertaken to investigate their structure-activity relationships. One compound was found to inhibit parasite growth in an in vitro assay and provides a lead to further develop 3-methylisoquinoline-4-carbonitriles as antimalarial compounds. Development of a potent and selective PfPKA inhibitor would provide a useful tool to shed further insight into the mechanisms enabling malaria parasites to establish infection.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Plasmodium falciparum / Proteínas Quinasas Dependientes de AMP Cíclico / Inhibidores de Proteínas Quinasas / Isoquinolinas / Nitrilos Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article País de afiliación: Australia Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Plasmodium falciparum / Proteínas Quinasas Dependientes de AMP Cíclico / Inhibidores de Proteínas Quinasas / Isoquinolinas / Nitrilos Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article País de afiliación: Australia Pais de publicación: Reino Unido