2. Academic Validation
  3. Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7

Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7

  • Bioorg Med Chem Lett. 2008 Oct 1;18(19):5294-8. doi: 10.1016/j.bmcl.2008.08.043.
Nathalie Bouloc 1,  Jonathan M Large,  Ela Smiljanic,  David Whalley,  Keith H Ansell,  Christopher D Edlin,  Justin S Bryans
Affiliations

Affiliation

  • 1 Drug Discovery Group, MRC Technology, 1-3 Burtonhole Lane, Mill Hill, London NW7 1AD, UK.
PMID: 18774709 DOI: 10.1016/j.bmcl.2008.08.043
Abstract

A high-throughput screening campaign identified a number of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7. Further synthetic chemistry efforts enabled the preparation of a number of analogues with promising in vitro potencies. Although these compounds show likely broad spectrum inhibitory activity, they represent a useful starting point for further chemical optimisation.

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