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Synthesis of hybrid anticancer agents based on kinase and histone deacetylase inhibitors

journal contribution
posted on 2023-06-08, 18:33 authored by Hiren Patel, Irina Chuckowree, Peter Coxhead, Matthew Guille, Minghua Wang, Alexandra Zuckermann, Robin S B Williams, Mariangela Librizzi, Ronald M Paranal, James E Bradner, John SpencerJohn Spencer
Fragments based on the VEGFR2i Semaxanib (SU5416, (vascular endothelial growth factor receptor-2 inhibitor) and the HDACi (histone deacetylase inhibitor) SAHA (suberanilohydroxamic acid) have been merged to form a range of low molecular weight dual action hybrids. Vindication of this approach is provided by SAR, docking studies, in vitro cancer cell line and biochemical enzyme inhibition data as well as in vivo Xenopus data for the lead molecule (Z)-N1-(3-((1H-pyrrol-2-yl)methylene)-2-oxoindolin-5-yl)- N8-hydroxyoctanediamide 6.

History

Publication status

  • Published

Journal

MedChemComm

ISSN

2040-2503

Publisher

Royal Society of Chemistry

Volume

5

Page range

1829-1833

Department affiliated with

  • Chemistry Publications

Full text available

  • Yes

Peer reviewed?

  • Yes

Legacy Posted Date

2014-09-30

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    University of Sussex (Publications)

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