Figure 1.
Structure of largazole-derivative OKI-006 and prodrugs OKI-005 and OKI-179. Largazole thiol was used a lead structure for medicinal chemistry optimization. Following identification of OKI-006, a first generation prodrug, OKI-005 was prepared and used for in vitro pharmacology studies. Subsequent prodrug optimization afforded OKI-179.
