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Synthesis and modeling of new benzofuranone histone deacetylase inhibitors that stimulate tumor suppressor gene expression.

Abstract：

:New benzofuranones were synthesized and evaluated toward NCI-H661 non-small cell lung cancer cells. Benzamide derivatives possessed micromolar antiproliferative and histone deacetylase inhibitory activities and modulate histone H4 acetylation. Hydroxamic acids were found to be potent nanomolar antiproliferative agents and HDAC inhibitors. Computational analysis presented a rationale for the activities of the hydroxamate derivatives. Impact of the HDAC inhibition on the expression of E-cadherin and the SEMA3F tumor suppressor genes revealed new promising compounds for lung cancer treatments.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Charrier C,Clarhaut J,Gesson JP,Estiu G,Wiest O,Roche J,Bertrand P

doi

10.1021/jm9002439

subject

Has Abstract

pub_date

2009-05-14 00:00:00

pages

3112-5

issue

9

eissn

0022-2623

issn

1520-4804

journal_volume

52

pub_type

杂志文章

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