Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity

This letter describes the development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved aqueous solubility (∼18 mg/mL) that translates into enhanced cell activity and caspase-3 induction.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry 2008, Vol.18 (1), p.49-53
Hauptverfasser:	Zhao, Zhijian, Robinson, Ronald G., Barnett, Stanley F., Defeo-Jones, Deborah, Jones, Raymond E., Hartman, George D., Huber, Hans E., Duggan, Mark E., Lindsley, Craig W.
Format:	Artikel
Sprache:	eng
Schlagworte:	Akt Antineoplastic agents Biological and medical sciences Cancer Caspase 3 - metabolism Cell Line, Tumor Enzyme Activation General aspects HT29 Cells Humans Inhibitors Kinases Kinetics Medical sciences Pharmacology. Drug treatments Phosphorylation Proto-Oncogene Proteins c-akt - antagonists & inhibitors Proto-Oncogene Proteins c-akt - metabolism Quinoxalines - chemical synthesis Quinoxalines - chemistry Quinoxalines - pharmacology Serine Proteinase Inhibitors - chemical synthesis Serine Proteinase Inhibitors - chemistry Serine Proteinase Inhibitors - pharmacology Solubility Water - chemistry
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Beschreibung
Zusammenfassung:	This letter describes the development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved aqueous solubility (∼18 mg/mL) that translates into enhanced cell activity and caspase-3 induction.
ISSN:	0960-894X 0968-0896 1464-3405 1464-3391
DOI:	10.1016/j.bmcl.2007.11.015