Total Synthesis of New Apicidin Derivatives as Potent Antitumor Agents

The antiparasitic agent apicidin, which was recently isolated from cultures of Fusarium Pallidoroseum, belongs to a rare group of cyclictetrapeptide fungal metabolites. Apicidin inhibits protozoal HDAC and is orally active against Plasmodium berghei malaria in mice. The biological activity of apicidin appears to be attributable to inhibition of apicomplexan HDAC at low nanomolar concentrations. In the present, we have worked about the synthesis of new apicidin derivatives and discovered that apicidin and some derivatives have mild antitumor activity. (omiited)