The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2H-pyran-4-yl)-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one)

ATM inhibitors, such as 7, have demonstrated the antitumor potential of ATM inhibition when combined with DNA double-strand break-inducing agents in mouse xenograft models. However, the properties of 7 result in a relatively high predicted clinically efficacious dose. In an attempt to minimize attri...

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Veröffentlicht in:	Journal of medicinal chemistry Jg. 61; H. 9; S. 3823 - 3841
Hauptverfasser:	Pike, Kurt G., Barlaam, Bernard, Cadogan, Elaine, Campbell, Andrew, Chen, Yingxue, Colclough, Nicola, Davies, Nichola L., de-Almeida, Camila, Degorce, Sebastien L., Didelot, Myriam, Dishington, Allan, Ducray, Richard, Durant, Stephen T., Hassall, Lorraine A., Holmes, Jane, Hughes, Gareth D., MacFaul, Philip A., Mulholland, Keith R., McGuire, Thomas M., Ouvry, Gilles, Pass, Martin, Robb, Graeme, Stratton, Natalie, Wang, Zhenhua, Wilson, Joanne, Zhai, Baochang, Zhao, Kang, Al-Huniti, Nidal
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	WASHINGTON Amer Chemical Soc 10.05.2018
Schlagworte:	Chemistry, Medicinal Life Sciences & Biomedicine Pharmacology & Pharmacy Science & Technology FREE-WILSON DESIGN STRAND BREAK REPAIR LIPOPHILIC EFFICIENCY DNA-DAMAGE RESPONSE PROTEIN-KINASE IN-VIVO HISTONE H2AX ABSORPTION CANCER
ISSN:	0022-2623, 1520-4804
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