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

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

Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche

Risultato della ricerca: Article › peer review

21 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 originale	English
pagine (da-a)	1829-1833
Numero di pagine	5
Rivista	MedChemComm
Volume	5
Stato di pubblicazione	Published - 2014

All Science Journal Classification (ASJC) codes

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???subjectarea.asjc.3000.3004???
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title = "Synthesis of hybrid anticancer agents based on kinase and histone deacetylase inhibitors",

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",

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

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language = "English",

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T1 - Synthesis of hybrid anticancer agents based on kinase and histone deacetylase inhibitors

AU - Librizzi, Mariangela

AU - Bradner, James E.

AU - Williams, Robin S. B.

AU - Coxhead, Peter

AU - Wang, Minghua

AU - Paranal, Ronald M.

AU - Librizzi, Mariangela

AU - Zuckermann, Alexandra

AU - Spencer, John

AU - Patel, Hiren

AU - Chuckowree, Irina

AU - Guille, Matthew

PY - 2014

Y1 - 2014

N2 - 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

AB - 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

UR - http://hdl.handle.net/10447/101733

M3 - Article

SN - 2040-2503

VL - 5

SP - 1829

EP - 1833

JO - MedChemComm

JF - MedChemComm

ER -

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

Abstract

All Science Journal Classification (ASJC) codes

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