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Issue 12, 2014
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Synthesis of hybrid anticancer agents based on kinase and histone deacetylase inhibitors

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Abstract

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.

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

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Publication details

The article was received on 15 May 2014, accepted on 16 Jun 2014 and first published on 18 Jun 2014


Article type: Concise Article
DOI: 10.1039/C4MD00211C
Med. Chem. Commun., 2014,5, 1829-1833

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

    H. Patel, I. Chuckowree, P. Coxhead, M. Guille, M. Wang, A. Zuckermann, R. S. B. Williams, M. Librizzi, R. M. Paranal, J. E. Bradner and J. Spencer, Med. Chem. Commun., 2014, 5, 1829
    DOI: 10.1039/C4MD00211C

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