A solid-phase synthetic route is described toward the natural product Spiruchostatin A and particularly its depsipeptidic, cysteine-containing analogs. After solid-phase preparation of linear precursors to these potential HDAC inhibitors, macrocyclization employing a latent thioester was used in an effort to generate the title compounds. The target depsipeptides are intended as potential treatments for cancer and other ailments implicating HDAC. The solid-phase route is designed for generating analogs that can be used to evaluate the influence of various residue side chains on HDAC binding and the resulting biological implications in transformed cells.

Spiruchostatin A and potential anticancer depsipeptidic analogs accessed via a latent thioester solid-phase route

248th National Meeting (2014)

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