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Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441.
TLDR
NU7441 shows sufficient proof of principle through in vitro and in vivo chemos Sensitization and radiosensitization to justify further development of DNA-PK inhibitors for clinical use. Expand
Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.
A solution-phase multiple-parallel synthesis approach was employed for the preparation of 6-, 7- and 8-aryl-substituted chromenone libraries, which were screened as inhibitors of the DNA repairExpand
Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles.
TLDR
CDK inhibition and chemosensitivity data indicate that the distinct mode of binding of NU2058 and NU6027 has direct consequences for enzyme and cell growth inhibition. Expand
2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-Dependent protein kinase (DNA-PK).
TLDR
Members of both structural classes were found to be selective inhibitors of DNA-PK over related phosphatidylinositol 3-kinase-related kinase (PIKK) family members. Expand
Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach.
TLDR
Structure-activity relationships for inhibition of DNA-dependent protein kinase (DNA-PK) have been defined and a number of 7-alkoxy-substituted chromen-4-ones displayed improved activity. Expand
Chemosensitization of Cancer Cells by KU-0060648, a Dual Inhibitor of DNA-PK and PI-3K
TLDR
The proof-of-principle in vitro and in vivo chemosensitization with KU-0060648 justifies further evaluation of dual DNA-PK and PI-3K inhibitors. Expand
Potentiation of anti-cancer agent cytotoxicity by the potent poly(ADP-ribose) polymerase inhibitors NU1025 and NU1064.
TLDR
The most suitable cytotoxic agents for use in combination with PARP inhibitors are methylating agents, bleomycin and ionizing radiation, but not anti-metabolites. Expand
Characterisation of a Tip60 Specific Inhibitor, NU9056, in Prostate Cancer
TLDR
Based on the activity of NU9056 and the specificity of the compound towards Tip60 relative to other HAT enzymes, these chemical biology studies have identified Tip60 as a potential therapeutic target for the treatment of prostate cancer. Expand
Structure-based design of a potent purine-based cyclin-dependent kinase inhibitor
TLDR
This work represents the first successful iterative synthesis of a potent CDK inhibitor based on the structure of fully activated CDK2–cyclin A, and the potency of O6-cyclohexylmethyl-2-(4′- sulfamoylanilino)purine was both predicted and fully rationalized on the basis of protein–ligand interactions. Expand
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