Identification of 6-Anilino Imidazo[4,5-c]pyridin-2-ones as Selective DNA-Dependent Protein Kinase Inhibitors and Their Application as Radiosensitizers

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Title

Identification of 6-Anilino Imidazo[4,5-c]pyridin-2-ones as Selective DNA-Dependent Protein Kinase Inhibitors and Their Application as Radiosensitizers

Content partner

The University of Auckland Library

Collection

ResearchSpace@Auckland

Description

The dominant role of non-homologous end-joining in the repair of radiation-induced double-strand breaks identifies DNA-dependent protein kinase (DNA-PK) as an excellent target for the development of radiosensitizers. We report the discovery of a new class of imidazo[4,5-c]pyridine-2-one DNA-PK inhibitors. Structure-activity studies culminated in the identification of 78 as a nM DNA-PK inhibitor with excellent selectivity for DNA-PK compared to related phosphoinositide 3-kinase (PI3K) and PI3K...

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Format

Research paper

Research format

Journal article

Creator

Hong, Cho R / Liew, Lydia P / Wong, Way W / Dickson, Benjamin D / Cheng, Gary / Shome, Avik / Airey, Rebecca / Jaiswal, Jagdish / Lipert, Barbara / Jamieson, Stephen MF / Wilson, William R / Hay, Michael P

URL

https://hdl.handle.net/2292/69826

Related subjects

Cell Line, Tumor / Animals / Humans / Mice / Mice, Nude / Rats / Imidazoles / Pyridones / Protein Kinase Inhibitors / Radiation-Sensitizing Agents / Xenograft Model Antitumor Assays / Structure-Activity Relationship / DNA-Activated Protein Kinase / 32 Biomedical and Clinical Sciences / 34 Chemical Sciences / 3211 Oncology and Carcinogenesis / Dental/Oral and Craniofacial Disease / Cancer / Colo-Rectal Cancer / Digestive Diseases / Rare Diseases / Orphan Drug / Radiation Oncology / 5.1 Pharmaceuticals / Science & Technology / Life Sciences & Biomedicine / Chemistry, Medicinal / Pharmacology & Pharmacy / SQUAMOUS-CELL CARCINOMA / CRYO-EM STRUCTURE / IONIZING-RADIATION / PLUS CETUXIMAB / SCID MUTATION / PK INHIBITOR / NECK-CANCER / POTENT / RADIOTHERAPY / HEAD / 0304 Medicinal and Biomolecular Chemistry / 0305 Organic Chemistry / 1115 Pharmacology and Pharmaceutical Sciences / 3214 Pharmacology and pharmaceutical sciences / 3404 Medicinal and biomolecular chemistry / 3405 Organic chemistry

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