Synthesis and Evaluation of HDAC Inhibitors Utilizing Intramolecular Acyl Transfer Activation

摘要

Extraordinary gene silencing of tumor suppressor genes is partly associated with histone hypoacetylation accompanying overexpression of HDAC proteins. Therefore, HDAC inhibitors have become a promising area of research in the development of selective drugs for the treatment of cancer. Psammaplin A is a symmetric disulfide containing natural product isolated from a marine sponge, and is reported as a prodrug form requiring reductive environment for releasing active thiol monomer (Psammaplin A-1) for HDAC inhibition.1