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

Attenni B, Ontoria JM, Cruz JC, Rowley M, Schultz-Fademrecht C, Steinkühler C, Jones P. Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model. Bioorg Med Chem Lett. 2009 Jun 1;19(11):3081-4. doi: 10.1016/j.bmcl.2009.04.011. Epub 2009 Apr 9. PMID: 19410459.

Histone deacetylase (HDAC) inhibitors represent a promising approach in cancer therapy by inducing hyperacetylation of histones, which triggers cell differentiation, growth arrest, and apoptosis in malignant cells. Many HDAC inhibitors currently in clinical trials feature a hydroxamic acid group, known for its potent zinc-binding properties that target various class I and class II HDAC isoforms. This study introduces a novel class I-selective HDAC inhibitor designed with a primary carboxamide group as its zinc-binding element. This innovative HDAC inhibitor demonstrates significant antiproliferative effects across multiple cancer cell lines and delivers therapeutic efficacy comparable to vorinostat in a xenograft model. By offering targeted action and strong anticancer potential, this compound highlights an exciting advancement in HDAC inhibitor development.

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