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

Synthesis and evaluation of metallocene containing methylidene-1,3-dihydro-2H-indol-2-ones as kinase inhibitors
Synthesis and evaluation of metallocene containing methylidene-1,3-dihydro-2H-indol-2-ones as kinase inhibitors
(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.
1756-5901
600-608
Spencer, John
a3cf55cd-a4c7-4af6-b16c-96c8fb8c4cf4
Amin, Jahangir
15a45a7a-1741-45fa-9f31-9aa6ef1924ed
Callear, Samantha K.
5af7f651-0ff0-4163-80b3-34996d62022a
Tizzard, Graham J.
8474c0fa-40df-43a6-a662-7f3c4722dbf2
Coles, Simon J.
3116f58b-c30c-48cf-bdd5-397d1c1fecf8
Coxhead, Peter
7d49795f-0a1b-416c-a61b-b367be46ae8d
Guille, Matthew
dfefb828-7c5b-4529-8df6-d7a10d8d5b67
Spencer, John
a3cf55cd-a4c7-4af6-b16c-96c8fb8c4cf4
Amin, Jahangir
15a45a7a-1741-45fa-9f31-9aa6ef1924ed
Callear, Samantha K.
5af7f651-0ff0-4163-80b3-34996d62022a
Tizzard, Graham J.
8474c0fa-40df-43a6-a662-7f3c4722dbf2
Coles, Simon J.
3116f58b-c30c-48cf-bdd5-397d1c1fecf8
Coxhead, Peter
7d49795f-0a1b-416c-a61b-b367be46ae8d
Guille, Matthew
dfefb828-7c5b-4529-8df6-d7a10d8d5b67

Spencer, John, Amin, Jahangir, Callear, Samantha K., Tizzard, Graham J., Coles, Simon J., Coxhead, Peter and Guille, Matthew (2011) Synthesis and evaluation of metallocene containing methylidene-1,3-dihydro-2H-indol-2-ones as kinase inhibitors. Metallomics, 3 (6), 600-608. (doi:10.1039/c1mt00017a).

Record type: Article

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.

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More information

Published date: 2011
Organisations: Organic Chemistry: Synthesis, Catalysis and Flow

Identifiers

Local EPrints ID: 346170
URI: http://eprints.soton.ac.uk/id/eprint/346170
ISSN: 1756-5901
PURE UUID: 4ce5a404-7c81-4c25-9293-c8b1f96a2e48
ORCID for Graham J. Tizzard: ORCID iD orcid.org/0000-0002-1577-5779
ORCID for Simon J. Coles: ORCID iD orcid.org/0000-0001-8414-9272

Catalogue record

Date deposited: 18 Dec 2012 12:04
Last modified: 15 Mar 2024 03:10

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Contributors

Author: John Spencer
Author: Jahangir Amin
Author: Samantha K. Callear
Author: Simon J. Coles ORCID iD
Author: Peter Coxhead
Author: Matthew Guille

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