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Bioorg Med Chem Lett. 2009 Jun 1;19(11):3081-4. doi: 10.1016/j.bmcl.2009.04.011. Epub 2009 Apr 9.

Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model.

Author information

1
IRBM/Merck Research Laboratories, Pomezia, Rome, Italy. thomas_e_barta@yahoo.com

Abstract

Histone deacetylase (HDAC) inhibition causes hyperacetylation of histones leading to differentiation, growth arrest and apoptosis of malignant cells, representing a new strategy in cancer therapy. Many of the known HDAC inhibitors (HDACi) that are in clinical trials possess a hydroxamic acid, that is a strong Zn(2+) binding group, thereby inhibiting some of the class I and class II isoforms. Herein we describe the identification of a selective class I HDAC inhibitor bearing a primary carboxamide moiety as zinc binding group. This HDACi displays good antiproliferative activity against multiple cancer cell lines, and demonstrates efficacy in a xenograft model comparable to vorinostat.

PMID:
19410459
DOI:
10.1016/j.bmcl.2009.04.011
[Indexed for MEDLINE]

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