Discovery of a Novel HDAC3 Selective Inhibitor and its Evaluation in Lymphoma Model

摘要

Histone deacetylase (HDAC) inhibition is a potentially attractive approach to cancer therapy. A number of HDAC inhibitors are in clinical development stages for the treatment of cancer as well as immune and inflammatory disorders. Although there are several approved HDAC inhibitors by the US FDA, they show a broad inhibitory spectrum against HDAC subfamily. Herein, we synthesized a series of novel hydroxamate analogs, and evaluated them with lymphoma cancer cell. Conclusively, we identified an HDAC3 selective inhibitor which shows good anticancer activity for the lymphoma model, as well as a good drug metabolism and pharmacokinetics (DMPK) profile.