Analogues of trichostatin A and trapoxin B as histone deacetylase inhibitors

Article abstract of DOI:10.1016/S0960-894X(97)00284-9

Inhibitors of histone deacetylase are potent inducers of differentiation and bear considerable potential as drugs for chemoprevention and treatment of cancer. So far only complex natural products and a few synthetic congeners have been identified as specific inhibitors. We have prepared a set of simple analogues in as little as four synthetic steps that have inhibitory potencies in the range of known cyclotetrapeptide inhibitors. These compounds are interesting leads for the design of potent inhibitors of histone deacetylase.