1357263-07-0Relevant articles and documents
SUBSTITUTED IMIDAZO[1,2-B]PYRIDAZINES
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Paragraph 0592-0595, (2013/08/28)
The invention relates to imidazo[1,2-b]pyridazines of general formula (I) a process for their manufacuture and their use for the treatment of benign and malignant neoplasia.
Diverse heterocyclic scaffolds as allosteric inhibitors of AKT
Kettle, Jason G.,Brown, Simon,Crafter, Claire,Davies, Barry R.,Dudley, Phillippa,Fairley, Gary,Faulder, Paul,Fillery, Shaun,Greenwood, Hannah,Hawkins, Janet,James, Michael,Johnson, Keith,Lane, Clare D.,Pass, Martin,Pink, Jennifer H.,Plant, Helen,Cosulich, Sabina C.
, p. 1261 - 1273 (2012/04/10)
Wide-ranging exploration of potential replacements for a quinoline-based inhibitor of activation of AKT kinase led to number of alternative, novel scaffolds with potentially improved potency and physicochemical properties. Examples showed predictable DMPK properties, and one such compound demonstrated pharmacodynamic knockdown of phosphorylation of AKT and downstream biomarkers in vivo and inhibition of tumor growth in a breast cancer xenograft model.