Synthesis and evaluation of metallocene containing methylidene-1,3-dihydro-2H-indol-2-ones as kinase inhibitors

John Spencer; Jahangir Amin; Samantha K. Callear; Graham J. Tizzard; Simon J. Coles; Peter Coxhead; Matthew Guille

doi:10.1039/C1MT00017A

Synthesis and evaluation of metallocene containing methylidene-1,3-dihydro-2H-indol-2-ones as kinase inhibitors†

John Spencer,*^a Jahangir Amin,^a Samantha K. Callear,^b Graham J. Tizzard,^b Simon J. Coles,^b Peter Coxhead^c and Matthew Guille ‡^c

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* Corresponding authors

^a School of Science, University of Greenwich at Medway, Central Avenue, Chatham, Kent, UK
E-mail: j.spencer@gre.ac.uk
Fax: +44 0208 331 9805

^b UK National Crystallography Service, School of Chemistry, University of Southampton, Highfield, UK

^c School of Biological Sciences, King Henry Building, University of Portsmouth, Portsmouth, UK

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.

Metallomics

Synthesis and evaluation of metallocene containing methylidene-1,3-dihydro-2H-indol-2-ones as kinase inhibitors†

Abstract

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