Research Topics
| Celine CanoSummaryAffiliation: University of Newcastle Country: UK Publications
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Detail Information
Publications
Atropisomeric 8-arylchromen-4-ones exhibit enantioselective inhibition of the DNA-dependent protein kinase (DNA-PK)Celine Cano
Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle upon Tyne, United KingdomNE1 7RU
Org Biomol Chem 8:1922-8. 2010..Biological evaluation against DNA-PK of the pairs of atropisomers showed a marked difference in potency, with only one enantiomer being biologically active...
DNA-dependent protein kinase (DNA-PK) inhibitors. Synthesis and biological activity of quinolin-4-one and pyridopyrimidin-4-one surrogates for the chromen-4-one chemotypeCeline Cano
Newcastle Cancer Centre, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle upon Tyne, UK
J Med Chem 53:8498-507. 2010....
Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivativesKate M Clapham
Newcastle Cancer Centre, Northern Institute for Cancer Research, School of Chemistry, Newcastle University, Newcastle upon Tyne, UK
Org Biomol Chem 10:6747-57. 2012..Biological evaluation against DNA-PK of each pair of atropisomers showed a marked difference in potency, with biological activity residing exclusively in the laevorotatory enantiomer...
Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3KJoanne M Munck
Medical School, Northern Institute for Cancer Research, Newcastle University, Framlington Place, Newcastle upon Tyne, NE2 4HH, United Kingdom
Mol Cancer Ther 11:1789-98. 2012..5-fold, without exacerbating etoposide toxicity to unacceptable levels. The proof-of-principle in vitro and in vivo chemosensitization with KU-0060648 justifies further evaluation of dual DNA-PK and PI-3K inhibitors...
Mapping the ATP-binding domain of DNA-dependent protein kinase (DNA-PK) with coumarin- and isocoumarin-derived inhibitorsSara L Payne
Northern Institute for Cancer Research, School of Chemistry, Newcastle University, Newcastle upon Tyne, UK
Bioorg Med Chem Lett 20:3649-53. 2010..Structure-activity relationships for DNA-PK inhibition were broadly consistent, albeit with a reduction of potency compared with the parent chromenone...
Versatile synthesis of functionalised dibenzothiophenes via Suzuki coupling and microwave-assisted ring closureSonsoles Rodriguez-Aristegui
Newcastle Cancer Centre, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle upon Tyne, United Kingdom NE1 7RU
Org Biomol Chem 9:6066-74. 2011..The data indicate permissive elaboration of hydroxyl at C-8 or C-9, enabling the possibility of improved pharmaceutical properties, whilst retaining potency against DNA-PK...
DNA-dependent protein kinase (DNA-PK) inhibitors: structure-activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domainKate M Clapham
Newcastle Cancer Centre, Northern Institute for Cancer Research, School of Chemistry, Newcastle University, Newcastle upon Tyne, United Kingdom
Bioorg Med Chem Lett 21:966-70. 2011....
Synthesis and biological evaluation of 5-substituted O4-alkylpyrimidines as CDK2 inhibitorsFrancesco Marchetti
Northern Institute for Cancer Research, Bedson Building, Newcastle University, Newcastle upon Tyne, UK NE1 7RU
Org Biomol Chem 8:2397-407. 2010..4 nM). The 5-formyl derivatives show selectivity for CDK2 over other CDK family members, and are growth inhibitory in tumour cells (e.g. 22j, GI(50) = 0.57 microM)...
8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK)Marine Desage-El Murr
Northern Institute for Cancer Research, School of Natural Sciences Chemistry, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, UK
Bioorg Med Chem Lett 18:4885-90. 2008....
Further characterisation of the cellular activity of the DNA-PK inhibitor, NU7441, reveals potential cross-talk with homologous recombinationMichele Tavecchio
Northern Institute for Cancer Research, School of Medical Sciences, Newcastle University, Paul O Gorman Building, Framlington Place, NE2 4HH Newcastle upon Tyne, UK
Cancer Chemother Pharmacol 69:155-64. 2012..One promising target is DNA-PK, a pivotal kinase in double-strand break repair. The purpose of this study was to further characterise the activity of the DNA-PK inhibitor NU7441, giving some new insights into the biology of DNA-PK...
Trifluoroethanol solvent facilitates selective N-7 methylation of purinesHonorine Lebraud
Newcastle Cancer Centre, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle upon Tyne, NE1 7RU, United Kingdom
Org Biomol Chem 11:1874-8. 2013..Subjecting the resulting cationic species to microwave irradiation releases an N(7)-methyl- or ethyl-purine. This one-pot procedure is an efficient regiospecific method applicable to diverse substrates...
