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

Mariangela Librizzi, James E. Bradner, Robin S. B. Williams, Peter Coxhead, Minghua Wang, Ronald M. Paranal, Mariangela Librizzi, Alexandra Zuckermann, John Spencer, Hiren Patel, Irina Chuckowree, Matthew Guille

Risultato della ricerca: Articlepeer review

19 Citazioni (Scopus)

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
Lingua originaleEnglish
pagine (da-a)1829-1833
Numero di pagine5
RivistaMedChemComm
Volume5
Stato di pubblicazionePublished - 2014

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

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