Bioorganic and Medicinal Chemistry p. 5766 - 5775 (2014)
Update date:2022-08-11
Topics:
Guan, Peng
Wang, Lei
Hou, Xuben
Wan, Yichao
Xu, Wenfang
Tang, Weiping
Fang, Hao
A series of 1,3,4-thiadiazole-containing hydroxamic acids, in accord with the common pharmacophore of histone deacetylase (HDAC) inhibitors (a Zn2+ binding moiety-a linker-a surface recognition motif), was identified as submicromolar HDAC inhibitors by our group. In this study, we continued our efforts to develop 1,3,4-thiadiazole bearing hydroxamate analogues by modifying the surface recognition motif. We found that 1,3,4-thiadiazoles having a heteroaromatic substituent showed better HDAC inhibitory activity in enzymatic assay and higher antiproliferative potency in cellular assay compared to SAHA.
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