7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: Design, synthesis, and biological activity

Autor:	Catherine A. Rugg, Angel R. Fuentes-Pesquera, Steven A. Middleton, Stuart Emanuel, Peter J. Connolly, Richard S. Alexander, Terry V. Hughes, Prabha Karnachi, Harold R. O’Grady
Rok vydání:	2008
Předmět:	Models Molecular Indoles Stereochemistry Clinical Biochemistry Aurora B kinase Pharmaceutical Science Protein Serine-Threonine Kinases Biochemistry Chemical synthesis Mice Structure-Activity Relationship Aurora Kinases Drug Discovery Animals Combinatorial Chemistry Techniques Molecular Biology Aurora Kinase A Molecular Structure biology Bicyclic molecule Vascular Endothelial Growth Factors Kinase Chemistry Organic Chemistry Receptor Protein-Tyrosine Kinases Kinase insert domain receptor Biological activity Xenograft Model Antitumor Assays Enzyme inhibitor Drug Design biology.protein Molecular Medicine Signal transduction
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 18:5130-5133
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2008.07.090
Popis:	A novel series of 7-[1H-indol-2-yl]-2,3-dihydro-isoindol-1-ones designed to be inhibitors of VEGF-R2 kinase was synthesized and found to potently inhibit VEGF-R2 and Aurora-A kinases. The structure-based design, synthesis, and initial SAR of the series are discussed.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::74affa60ae9f6997d3605a0b25abe5da https://doi.org/10.1016/j.bmcl.2008.07.090 Zobrazit plný text záznamu Full Text from ScienceDirect