Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 22, Issue 21, Pages 5766-5775Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.09.039
Keywords
1,3,4-Thiadiazole; Hydroxamic acid; Histone deacetylase inhibitor; Surface recognition motif; Antiproliferation
Funding
- National Natural Science Foundation China [81373281]
- Shandong Natural Science Fund for Distinguished Young Scholars [JQ201319]
- Program for New Century Excellent Talents in University [NCET-12-0337]
- Independent Innovation Foundation of Shandong University, IIFSDU [2012JC003]
- Program for Changjiang Scholars and Innovative Research Team in University, PCSIRT [IRT13028]
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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. (C) 2014 Elsevier Ltd. All rights reserved.
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