Despite major advances in cancer treatment strategies in recent years, significant limitations still remain. Selectively targeting cancer cells without affecting normal cells is a challenging task. Histone deacetylase (HDAC) enzymes, which are overexpressed in many cancer tissues, provide a potential target for cancer chemotherapy. Therefore, HDAC inhibitors (HDACis) are currently being widely investigated as anticancer agents. Most of the current HDACis are not selective and have undesirable side effects. Selective inhibition of specific HDAC isoforms to preferentially suppress the proliferation of cancer cells is a goal yet to be achieved.<br/>Most of current clinically used HDAC inhibitors have hydroximic acid as the zinc-binding group. We used molecular modeling studies to design a new class of HDAC inhibitors with a novel zinc-binding group. Some of these compounds showed higher cell growth inhibition than the FDA approved drug vorinostat (SAHA) and showed mitotic arrest in the cell inhibition assay. The design, synthesis, and biological activity of these compounds will be presented.<br/>

Design, synthesis, and biological evaluation of novel histone deacetylase inhibitors as anti-cancer agents

254th National Meeting (2017)

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