several human cyclin-dependent kinase inhibitors, structurally related to roscovitine, as new anti-malarial agents

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ID: 253378
2014
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Abstract
In Africa, malaria kills one child each minute. It is also responsible for about one million deaths worldwide each year. Plasmodium falciparum, is the protozoan responsible for the most lethal form of the disease, with resistance developing against the available anti-malarial drugs. Among newly proposed anti-malaria targets, are the P. falciparum cyclin-dependent kinases (PfCDKs). There are involved in different stages of the protozoan growth and development but share high sequence homology with human cyclin-dependent kinases (CDKs). We previously reported the synthesis of CDKs inhibitors that are structurally-related to (R)-roscovitine, a 2,6,9-trisubstituted purine, and they showed activity against neuronal diseases and cancers. In this report, we describe the synthesis and the characterization of new CDK inhibitors, active in reducing the in vitro growth of P. falciparum (3D7 and 7G8 strains). Six compounds are more potent inhibitors than roscovitine, and three exhibited IC50 values close to 1 µM for both 3D7 and 7G8 strains. Although, such molecules do inhibit P. falciparum growth, they require further studies to improve their selectivity for PfCDKs.
Reference Key
houz2014moleculesseveral Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors ;Sandrine Houzé;Nha-Thu Hoang;Olivier Lozach;Jacques Le Bras;Laurent Meijer;Hervé Galons;Luc Demange
Journal Journal of ethnopharmacology
Year 2014
DOI
10.3390/molecules190915237
URL
http://www.mdpi.com/1420-3049/19/9/15237
Keywords
2 plasmodium falciparum

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