Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model

Autor:	Deborah Defeo-Jones, Anthony M. Smith, Ronald G. Robinson, Mark T. Bilodeau, Stanley F. Barnett, George D. Hartman, Raymond E. Jones, Karen R. Leander, Jacob M. Hoffman, Peter J. Manley, Adrienne E. Balitza, Kathleen M. Haskell, Hans E. Huber
Rok vydání:	2008
Předmět:	Clinical Biochemistry Allosteric regulation Pharmaceutical Science AKT2 Antineoplastic Agents Biochemistry Mice Structure-Activity Relationship In vivo Drug Discovery Animals Combinatorial Chemistry Techniques Humans Naphthyridines Molecular Biology Protein kinase B biology Kinase Chemistry Organic Chemistry In vitro Disease Models Animal Enzyme inhibitor Drug Design embryonic structures Cancer research biology.protein Molecular Medicine Signal transduction Drug Screening Assays Antitumor Proto-Oncogene Proteins c-akt
Zdroj:	Bioorganicmedicinal chemistry letters. 18(11)
ISSN:	1464-3405
Popis:	A series of naphthyridine and naphthyridinone allosteric dual inhibitors of Akt1 and 2 have been developed. These compounds have been optimized to have potent dual activity against the activated kinase as well as the activation of Akt in cells. One molecule in particular, compound 17, has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d0a639621144e65e5990ceb0f62ca51f https://pubmed.ncbi.nlm.nih.gov/18479914 Zobrazit plný text záznamu Full Text from ScienceDirect