Design, synthesis and preliminary bioactivity studies of 1,3,4-thiadiazole hydroxamic acid derivatives as novel histone deacetylase inhibitors

Bioorganic & Medicinal Chemistry
Peng GuanHao Fang

Abstract

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 (IC(50) = 0.089 μM), exhibited better inhibitory effect compared with SAHA (IC(50) = 0.15 μM).

References

Jan 7, 2006·Nature Reviews. Cancer·Saverio Minucci, Pier Giuseppe Pelicci
Sep 7, 2006·Nature Reviews. Drug Discovery·Jessica E BoldenRicky W Johnstone

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Citations

Sep 2, 2014·Chemical & Pharmaceutical Bulletin·Feng RenNa Jin
Jul 26, 2016·BMC Pharmacology & Toxicology·Yan-Xin HuangYu-Xin Li
May 11, 2018·Anti-cancer Agents in Medicinal Chemistry·Mehlika D AltıntopZafer A Kaplancıklı
Oct 3, 2017·SAR and QSAR in Environmental Research·M ManalM J N Chandrasekar
Sep 4, 2020·Pharmacological Reports : PR·Monika Szeliga
Aug 20, 2019·Bioorganic & Medicinal Chemistry·Patrick M WehrliJohan Gottfries
Jul 7, 2021·Bioorganic Chemistry·Christiana MantzouraniGeorge Kokotos

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