Synthesis and phosphatase inhibitory activity of analogs of sulfircin

Analogs of sulfircin (1) were synthesized and tested for inhibitory activity against a panel of phosphatases. We attempted to optimize the potency and selectivity of sulfircin for Cdc25A by modifying three structural areas of the molecule. An anionic group is required for potency and malonate was found to be an effective substitute for sulfate.

The synthesis of structural analogs of sulfircin (1) is described. The compounds are tested for activity against Cdc25 as well as selectivity against a panel of other phosphatases.Figure optionsDownload as PowerPoint slide