Bioorganic & Medicinal Chemistry Letters 2004-11-01

Novel histone deacetylase inhibitors: cyclic tetrapeptide with trifluoromethyl and pentafluoroethyl ketones.

Binoy Jose, Yusuke Oniki, Tamaki Kato, Norikazu Nishino, Yuko Sumida, Minoru Yoshida

Index: Bioorg. Med. Chem. Lett. 14(21) , 5343-6, (2004)

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Abstract

Cyclic tetrapeptides containing trifluoromethyl and pentafluoroethyl ketone as zinc binding functional group were synthesized as potent HDAC inhibitors. Evaluation by human HDAC inhibition assay and p21 promoter assay showed that these inhibitors are promising anticancer agents.