1357159-32-0Relevant academic research and scientific papers
NRF2 REGULATORS
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, (2015/07/07)
The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.
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.
