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Updated: Jan 8, 2026

Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS
Published on: August 10, 2017
A comprehensive review on azole-based hydroxamic acid analogs as histone deacetylases (HDACs) inhibitors
Deepali Shukla1, Balaji Wamanrao Matore1, Anjali Murmu1
1Laboratory of Drug Discovery and Ecotoxicology, Department of Pharmacy, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur, India.
Background:
Histone deacetylases (HDAC) are essential epigenetic enzymes that modulate the remodeling of chromatin and transcriptional activity. Overexpression of HDAC has been associated with tumorigenesis, angiogenesis, metastasis, and therapeutic resistance.
Methods:
A systematic survey (2008-2025) evaluated the design, mechanism, and structure-activity relationships (SAR) of azole-based hydroxamic acid (ABHA) derivatives as histone deacetylase inhibitors (HDACIs).
Results:
ABHAs containing 1,3,4-oxadiazole, pyrazole, imidazole, triazole, indazole, thiadiazole, etc. Heterocyclic scaffolds show significant zinc-binding affinity, enhanced pharmacokinetics, and isoform-selective inhibition. Subtle structural variations in heteroaryl substituents, linker architecture, and hydroxamate coordination significantly modulate enzyme selectivity and cytotoxic efficacy.
Conclusion:
ABHA hybrids provide versatile scaffolds with diverse activity for the rational development of next-generation, isoform-selective HDACIs with enhanced potency and therapeutic promise in anticancer drug design.
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