The development of new tumors and growing resistance to existing anticancer drugs has always been motivating research for new drug discovery. Histone deacetylase (HDAC) is found to be overexpressed in some cancer cells, which condenses the chromatin structure of tumor suppressor genes, cell-cycle inhibitor genes and apoptosis inducer genes. Four HDAC inhibitors, specifically Vorinostat, Romidepsin, Belinostat and Panobinostat, have been approved by FDA for cancer treatment. A newly designed HDAC inhibitor comprises of a main scaffold, a zinc-binding group, a protein recognition cap and also a coordination site to metal ions. The compound was synthesized through an amide coupling condensation reaction in anhydrous condition, followed by acidification, deprotection and a final neutralization step. The HDAC inhibitor has been characterized by MS and NMR analysis. Metal ions (Pt or Cu) could anchor at the coordination site of the inhibitor, resulting in bifunctional metal complexes. HDAC enzyme inhibition and cell viability studies of the inhibitor and its metal complexes will be examined.

Synthesis, characterization and reactivities of a new HDAC inhibitor

2019 Spring National Meeting

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