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Mapping the ATP-binding domain of DNA-dependent protein kinase (DNA-PK) with coumarin- and isocoumarin-derived inhibitors.
Replacement of the core heterocycle of a defined series of chromen-4-one DNA-PK inhibitors by the isomeric chromen-2-one (coumarin) and isochromen-1-one (isocoumarin) scaffolds was investigated.Expand
Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor.
TLDR
The optimization of imidazo [1,2-a] pyrazines is described, which allow us to identify compound 14 (ETP-46321), with potent biochemical and cellular activity and good pharmacokinetic properties (PK) after oral dosing. Expand
Imidazo[1,2-a]pyrazines as novel PI3K inhibitors.
TLDR
A novel series of imidazo[1,2-a]pyrazines as PI3K inhibitors is described as an important target for cancer therapeutics due to the deregulation of its signaling pathway in a wide variety of human cancers. Expand
Identification of potent water-soluble DNA-dependent protein kinase (DNA-PK) inhibitors using a small-molecule library approach [abstract]
4156 The clinical response to DNA-damaging anticancer therapies may be compromised by cellular DNA repair processes, and agents that impede DNA repair are thus of potential therapeutic interest asExpand
Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
TLDR
A novel chemical series of triazolo[4,3-b]pyridazine based tricycles is generated by applying a scaffold hopping strategy over the authors' previously reported potent pan-PIM inhibitor ETP-47453 (compound 2), demonstrating a rather selective PIM-1/PIM-3 biochemical profile. Expand
Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy.
TLDR
A further exploration of the lead PI3K inhibitor ETP-46321 is reported by the application of a conformational restriction strategy and novel tricyclic imidazo[1,2-a]pyrazine derivatives asPI3K inhibitors are synthesized. Expand
Versatile synthesis of functionalised dibenzothiophenes via Suzuki coupling and microwave-assisted ring closure.
TLDR
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. Expand
New use of bis(benzotriazolyl)-1,2-(dialkylamino)ethanes for the synthesis of 2-H-3-dialkylamino imidazo[1,2-a]pyrazine derivatives
Abstract First direct synthesis of 2- H -3- N -dialkyl-imidazo[1,2- a ]pyrazines is described. This approach makes use of accessible substituted pyrazines and the assistance of benzotriazole. In suchExpand