Design, synthesis and biological evaluation of novel compounds with conjugated structure as anti-tumor agents

A series of hydroxamic acids with conjugated structure was designed and synthesized to explore the possible HDAC subtype selectivity by testing these compounds against recombinant human HDAC1 and HDAC4. The most selective compound resulted 5a, with a SI of 11.9. The enzymatic inhibitory activity of these conjugated compounds was relatively weak; however, some of these compounds showed significant effect in inducing apoptosis. Moreover, the anti-proliferative activity in cancer cells resulted quite promising, especially in the HCT119 cell line.

A series of hydroxamic acids with conjugated stereodefined structure were designed as HDAC inhibitors.Figure optionsDownload as PowerPoint slide