- The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5- a]pyridin-6-yl)amino]-9-(tetrahydro-2 H-pyran-4-yl)-7,9-dihydro-8 H-purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor
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DNA-PK is a key component within the DNA damage response, as it is responsible for recognizing and repairing double-strand DNA breaks (DSBs) via non-homologous end joining. Historically it has been challenging to identify inhibitors of the DNA-PK catalyti
- Goldberg, Frederick W.,Finlay, M. Raymond V.,Ting, Attilla K. T.,Beattie, David,Lamont, Gillian M.,Fallan, Charlene,Wrigley, Gail L.,Schimpl, Marianne,Howard, Martin R.,Williamson, Beth,Vazquez-Chantada, Mercedes,Barratt, Derek G.,Davies, Barry R.,Cadogan, Elaine B.,Ramos-Montoya, Antonio,Dean, Emma
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supporting information
p. 3461 - 3471
(2020/02/04)
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- A convenient synthesis of linear pyridinoimidazo[1,2-a]pyridine and pyrroloimidazo[1,2-a]pyridine cores
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Two new imidazo[1,2-a]pyridine derivatives, pyridinoimidazo[1,2-a]pyridine (10) and pyrroloimidazo[1,2-a]pyridine (16), were synthesised from 2-amino-4-methyl-5-nitropyridine (1) by linear cyclisation, making use of dimethylformamide dimethylacetal (DMFDMA) as an agent of vinylamine functionalisation. This report describes first the formation of pyridine and pyrroloimidazopyridine from (1), and then the formation of pyridine-fused and pyrrolo-fused pyridine by the Friedl?nder method and reductive cyclisation followed by treatment of the resulting adduct with chloroacetaldehyde.
- Andaloussi, Mounir,Moreau, Emmanuel,Chavignon, Olivier,Teulade, Jean C.
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p. 8392 - 8395
(2008/03/14)
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