Design, synthesis and preliminary bioactivity studies of 1,3,4-thiadiazole hydroxamic acid derivatives as novel histone deacetylase inhibitors
2012
Guan, Peng | Sun, Feng’e | Hou, Xuben | Wang, Feng | Yi, Fan | Xu, Wenfang | Fang, Hao
Histone deacetylase (HDAC) inhibitors have emerged as a new class of anticancer agents, targeting the biological processes including cell cycle, apoptosis and differentiation. In the present study, a series of 1,3,4-thiadiazole based hydroxamic acids were developed as potent HDAC inhibitors. Some of them showed good inhibitory activity in HDAC enzyme assay and potent growth inhibition in some tumor cell lines. Among them, compound 6i (IC₅₀=0.089μM), exhibited better inhibitory effect compared with SAHA (IC₅₀=0.15μM).
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