Design and synthesis of novel histone deacetylase 6 inhibitors with benzyl-triazole as the core skeleton.

In this study, we designed and synthesized twenty-seven novel hydroxamic acid-based HDAC inhibitors (HDACis) with benzyl-triazole as the core skeleton. Most target compounds displayed excellent inhibition rates toward HDACs. Among them, compounds ZM-22 to ZM-27 with inhibition rates more than 90% toward HDACs exhibited potent inhibitory activity toward HDAC6, and ZM-23 possessed the best selectivity to HDAC6 over HDAC1. The high potency of compound ZM-23 toward HDAC6 was rationalized by molecular docking simulation. This series of compounds is worthy for further anti-cancer activity evaluation and structural optimization works. PMID: 31155552 [PubMed - as supplied by publisher]
Source: BioScience Trends - Category: Biomedical Science Tags: Biosci Trends Source Type: research