Potent and Orally Effcacious Bisthiazole-Based Histone Deacetylase Inhibitors

摘要

Inspired by the thiazole-thiazoline cap group in natural product largazole, a series of structurally simpli?ed bisthiazole-based histone deacetylase inhibitors were prepared and evaluated. Compound 8f was evaluated in vivo in an experimental autoimmune encephalomyelitis (EAE) model and found to be orally effcacious in ameliorating clinical symptoms of EAE mice.