| Literature DB >> 22248236 |
Jason G Kettle1, Simon Brown, Claire Crafter, Barry R Davies, Phillippa Dudley, Gary Fairley, Paul Faulder, Shaun Fillery, Hannah Greenwood, Janet Hawkins, Michael James, Keith Johnson, Clare D Lane, Martin Pass, Jennifer H Pink, Helen Plant, Sabina C Cosulich.
Abstract
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.Entities:
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Year: 2012 PMID： 22248236 DOI： 10.1021/jm201394e
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446