Recently, we reported that the natural product derrubone exhibits Hsp90 inhibitory activity. Due to itsunique architectural scaffold and proposed rapid assembly, the synthesis of this natural product waspursued with the aim of identifying structure-activity relationships. Synthesis of the natural productwas accomplished in eight highly convergent steps, which led to a facile method for the construction ofrelated compounds. Biological evaluation of derrubone and its analogues identified several compoundsthat exhibit low micromolar inhibitory activity against breast and colon cancer cell lines.
