Design of N-substituted Amino Caproic Hydroxamic Acid Histone Deacetylase Inhibitors Reveal an Essential Role for Cap Atomic Composition

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
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Design of N-substituted Amino Caproic Hydroxamic Acid Histone Deacetylase Inhibitors Reveal an Essential Role for Cap Atomic Composition



Anti-Cancer Agents in Medicinal Chemistry, 12(7): 801-806.

Author(s): Jean M. Brunel, Chanaz Salmi-Smail, Audrey Restouin, Thomas Prebet, Norbert Vey and Yves Collette.

Affiliation: Aix-Marseille Universite, Centre de Recherche en Cancerologie de Marseille (CRCM), Laboratory of Integrative Structural & Chemical Biology (iSCB), UMR CNRS 7258, Inserm-U1068, Faculte de Pharmacie, 27 Bd Jean Moulin, 13385 Marseille Cedex 05, France.

Abstract

A series of N-substituted amino caproic hydroxamic acid histone deacetylase inhibitors derivatives was designed in good-toexcellent yields and evaluated for their antiproliferative activity in a panel of human cancer cell lines, showing half maximum effective concentration varying from 700 nM to > 100 μM. Interestingly, the replacement of a furyl group by a thienyl one impacted very significantly the cap role on this antiproliferative activity and on histone acetylation induced by these drugs in cell-based but also in cell-free enzyme assays, suggesting an important role of the electronic density attached to the oxygen or sulfur atoms.

Keywords:

N-substituted amino caproic hydroxamic acid, Histone deacetylase inhibitors, Anticancer agents, SAHA derivatives, carcinogenesis, dichloromethane, chromatography, aminohexanoic.



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Article Details

Volume: 12
Issue Number: 7
First Page: 801
Last Page: 806
Page Count: 6
DOI: 10.2174/187152012802650192
Price: $58
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