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; Librizzi, Mariangela; Paranal, Ronald M.; Bradner, James E.; Spencer, John.

In: MedChemComm, Vol. 12, 01.12.2014, p. 1829-1833.

Research output: Contribution to journalArticlepeer-review

Published

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.
Original languageEnglish
Pages (from-to)1829-1833
Number of pages5
JournalMedChemComm
Volume12
DOIs
Publication statusPublished - 1 Dec 2014
This open access research output is licenced under a Creative Commons Attribution-NonCommercial-NoDerivs 3.0 Unported License.

ID: 22649937