Now showing items 1-3 of 3

  • Discovery of N-Phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors 

    Wang, S.; Midgley, C. A.; Scaërou, F.; Grabarek, J. B.; Griffiths, G.; Jackson, W.; Kontopidis, G.; McClue, S. J.; McInnes, C.; Meades, C.; Mezna, M.; Plater, A.; Stuart, I.; Thomas, M. P.; Wood, G.; Clarke, R. G.; Blake, D. G.; Zheleva, D. I.; Lane, D. P.; Jackson, R. C.; Glover, D. M.; Fischer, P. M. (2010)
    Through cell-based screening of our kinase-directed compound collection, we discovered that a subset of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amines were potent cytotoxic agents against cancer cell lines, suppressed mitotic ...
  • REPLACE: A strategy for iterative design of cyclin-binding groove inhibitors 

    Andrews, M. J. I.; Kontopidis, G.; McInnes, C.; Plater, A.; Innes, L.; Cowan, A.; Jewsbury, P.; Fischer, P. M. (2006)
    We describe a drug-design strategy termed REPLACE (REplacement with Partial Ligand Alternatives through Computational Enrichment) in which nonpeptidic surrogates for specific determinants of known peptide ligands are ...
  • Truncation and optimisation of peptide inhibitors of cyclin-dependent kinase 2-cyclin A through structure-guided design 

    Kontopidis, G.; Andrews, M. J.; McInnes, C.; Plater, A.; Innes, L.; Renachowski, S.; Cowan, A.; Fischer, P. M. (2009)
    The cyclin-dependent kinase 2-cyclin A complex is an important regulator of the DNA-synthesis phase of the mammalian cell cycle, which is frequently deregulated in cancer. Rather than blocking the ATP-binding site of the ...