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

Patel, Hiren, Chuckowree, Irina, Coxhead, Peter, Guille, Matthew, Wang, Minghua, Zuckermann, Alexandra, Williams, Robin S B, Librizzi, Mariangela, Paranal, Ronald M, Bradner, James E and Spencer, John (2014) Synthesis of hybrid anticancer agents based on kinase and histone deacetylase inhibitors. MedChemComm, 5. pp. 1829-1833. ISSN 2040-2503

[img]
Preview
PDF
Download (343kB) | Preview

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.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Subjects: Q Science
Depositing User: Deeptima Massey
Date Deposited: 30 Sep 2014 10:16
Last Modified: 07 Mar 2017 09:17
URI: http://sro.sussex.ac.uk/id/eprint/50416

View download statistics for this item

📧 Request an update