title: Synthesis and evaluation of metallocene containing methylidene-1,3-dihydro-2H-indol-2-ones as kinase inhibitors.
abstract: (E)- and (Z)-3-Ferrocenylmethylidene-1,3-dihydro-2H-indol-2-ones 1 have been structurally modified in order to explore SAR against a range of kinases. Of note is the submicromolar to low micromolar inhibition of DYRK3 and 4 by a number of complexes. Screening using Xenopus embryos showed some of the compounds to have potent antiangiogenisis activity.
authors.affiliation: School of Science, University of Greenwich at Medway, Central Avenue, Chatham, Kent, ME4 4TB, UK. j.spencer@gre.ac.uk
authors.forename: John
authors.initials: J
authors.lastname: Spencer
authors.forename: Jahangir
authors.initials: J
authors.lastname: Amin
authors.forename: Samantha K
authors.initials: SK
authors.lastname: Callear
authors.forename: Graham J
authors.initials: GJ
authors.lastname: Tizzard
authors.forename: Simon J
authors.initials: SJ
authors.lastname: Coles
authors.forename: Peter
authors.initials: P
authors.lastname: Coxhead
authors.forename: Matthew
authors.initials: M
authors.lastname: Guille
mesh_terms: D000818:Animals; D018360:Crystallography, X-Ray; D004625:Embryo, Nonmammalian / Q000187:drug effects / Q000196:embryology / Q000201:enzymology; D017403:In Situ Hybridization; D008956:Models, Chemical; D008958:Models, Molecular; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D040281:Vascular Endothelial Growth Factor Receptor-1 / Q000037:antagonists & inhibitors / Q000235:genetics; D029867:Xenopus Proteins / Q000037:antagonists & inhibitors / Q000235:genetics; D014982:Xenopus laevis / Q000196:embryology
chemical_list: D009942:Organometallic Compounds; D047428:Protein Kinase Inhibitors; D029867:Xenopus Proteins; C013108:metallocene; D040281:Vascular Endothelial Growth Factor Receptor-1