Auflistung nach Autor "Fischer, P. M."
Anzeige der Dokumente 1-6 von 6
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4-Arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects
Kryštof, V.; Cankař, P.; Fryšová, I.; Slouka, J.; Kontopidis, G.; Džubák, P.; Hajdúch, M.; Srovnal, J.; De Azevedo Jr, W. F.; Orság, M.; Paprskářová, M.; Rolčík, J.; Látr, A.; Fischer, P. M.; Strnad, M. (2006)In a routine screening of our small-molecule compound collection we recently identified 4-arylazo-3,5-diamino-1H-pyrazoles as a novel group of ATP antagonists with moderate potency against CDK2-cyclin E. A preliminary SAR ... -
Design, synthesis, and evaluation of 2-methyl- and 2-amino-N-aryl-4,5- dihydrothiazolo[4,5-h]quinazolin-8-amines as ring-constrained 2-anilino-4-(thiazol-5-yl)pyrimidine cyclin-dependent kinase inhibitors
McIntyre, N. A.; McInnes, C.; Griffiths, G.; Barnett, A. L.; Kontopidis, G.; Slawin, A. M. Z.; Jackson, W.; Thomas, M.; Zheleva, D. I.; Wang, S.; Blake, D. G.; Westwood, N. J.; Fischer, P. M. (2010)Following the recent discovery and development of 2-anilino-4-(thiazol-5- yl)pyrimidine cyclin dependent kinase (CDK) inhibitors, a program was initiated to evaluate related ring-constrained analogues, specifically, 2-methyl- ... -
Discovery and characterization of 2-anilino-4- (thiazol-5-yl)pyrimidine transcriptional CDK inhibitors as anticancer agents
Wang, S.; Griffiths, G.; Midgley, C. A.; Barnett, A. L.; Cooper, M.; Grabarek, J.; Ingram, L.; Jackson, W.; Kontopidis, G.; McClue, S. J.; McInnes, C.; McLachlan, J.; Meades, C.; Mezna, M.; Stuart, I.; Thomas, M. P.; Zheleva, D. I.; Lane, D. P.; Jackson, R. C.; Glover, D. M.; Blake, D. G.; Fischer, P. M. (2010)The main difficulty in the development of ATP antagonist kinase inhibitors is target specificity, since the ATP-binding motif is present in many proteins. We introduce a strategy that has allowed us to identify compounds ... -
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 ...