A New Simple and High-Yield Synthesis of Suberoylanilide Hydroxamic Acid and Its Inhibitory Effect Alone or in Combination with Retinoids on Proliferation of Human Prostate Cancer Cells

摘要

We have developed a procedure for the synthesis of N-hydroxy-N~1-phenyloctanediamide (suberoylanilide hydroxamic acid (SAHA)),providing the product in 79.8% yield.SAHA is a potent inhibitor of histone deacetylase,induces differentiation and/or apoptosis in certain transformed cells in culture,and suppressed the growth of human prostate cancer LNCaP and PC-3 cell lines.The combination of SAHA with other compounds inhibited cell proliferation of LNCaP cells in additive fashion and resulted in synergistic growth inhibition.