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Hydrazides as Potential HDAC Inhibitors: Structure-activity Relationships and Biological Implications
Suvankar Banerjee1, Sandip Kumar Baidya1, Nilanjan Adhikari1
1Natural Science Laboratory, Division of Medicinal and Pharmaceutical Chemistry, Department of Pharmaceutical Technology, P.O. Box 17020, Jadavpur University, Kolkata, 700032, West Bengal, India.
Current Topics in Medicinal Chemistry
|April 11, 2023
Summary
Histone deacetylase (HDAC) inhibitors show promise for treating diseases but cause toxicity. Hydrazide-based compounds offer specific HDAC selectivity, paving the way for safer drug development.
Area of Science:
- Biochemistry
- Pharmacology
- Medicinal Chemistry
Background:
- Epigenetic regulation by histone deacetylases (HDACs) is crucial in various diseases, including cancers, neurodegenerative, inflammatory, and metabolic disorders.
- Current HDAC inhibitors face limitations due to broad-spectrum activity, toxicity, and off-target effects, necessitating improved selectivity.
Purpose of the Study:
- To elucidate the detailed structure-activity relationship (SAR) of existing hydrazide-based HDAC inhibitors.
- To provide insights for developing novel HDAC inhibitors with enhanced specificity and reduced toxicity.
Main Methods:
- Review and analysis of existing literature on hydrazide-based HDAC inhibitors.
- Detailed examination of structure-activity relationships (SAR) within this compound class.
Main Results:
- Hydrazide-based compounds demonstrate significant inhibitory efficacy and high selectivity for specific HDAC targets.
- SAR analysis reveals key structural features contributing to potent and selective HDAC inhibition.
Conclusions:
- Hydrazide-based compounds represent a promising scaffold for developing targeted HDAC inhibitors.
- Further exploration of SAR can lead to the creation of safer and more effective therapeutic agents for various diseases.
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