Bioorganic & Medicinal Chemistry Letters 2012-11-01

Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases.

Md Ashraful Hoque, Toru Arai, Norikazu Nishino, Hyun-Jung Kim, Akihiro Ito, Minoru Yoshida

Index: Bioorg. Med. Chem. Lett. 22(21) , 6770-2, (2012)

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Abstract

Two thioacetate tails were introduced to the chlamydocin- and CHAP31-related cyclic tetrapeptides. An intramolecular disulfide bridge could be formed in the CHAP31-related cyclic peptides. Both the thioacetate-tailed and disulfide-bridged peptides were potent histone deacetylase inhibitors in the presence of sulfhydryl compound. Potent p21 promoter inducing activity was also observed in vivo.Copyright © 2012. Published by Elsevier Ltd.