O

Valproic acid

3.2.2. Hydroxamic acids

The hydroxamic acid function is a potent zinc chelator, as previously mentioned in the context of matrix metalloproteinase inhibitors (Section 2.1), and some potent inhibitors of HDAC belong to this class of compounds. Trichostatin A (TSA), a natural product isolated from Streptomyces hygroscopicus, was first shown to be a potent inducer of cell differentiation and cell cycle arrest, and later reported to have anti-HDAC activity. It is still in preclinical studies.77 Vorinostat (suberoyla-nilide hydroxamic acid, SAHA) was the first member of this class to enter human clinical trials78 and has been approved by the FDA for cutaneous T-cell lymphoma (CTCL) for patients who have progressive, persistent, or recurrent disease or following failure of two systemic therapies, making the oral drug the first HDAC inhibitor to reach the market. Pyroxamide, a bioisoster of vorinostat, is also under clinical assays in patients with advanced malignancies.79 Several hydroxamic derivatives of cinnamic acid, such as PDX-101, LBH-589,80 and NVP-LAQ-824, are also under clinical evaluation for hematological and solid tumors.

CH3 CH3 Trichostatin A (TSA) O

aoso ch3

CH3 CH3 Trichostatin A (TSA) O

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