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Updated: Sep 18, 2025

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Benzamide-Containing Histone Deacetylase Inhibitors With Anticancer Therapeutic Potential
Juntao Song1, Shujing Si2, Jie Qin2
1Hematology & Oncology Department, Zibo 148 Hospital, China RongTong Medical Healthcare Group Co. Ltd., Zibo, Shandong Province, People's Republic of China.
Abstract:
Histone deacetylases (HDACs) could regulate gene expression, arrest the cell cycle, alter epigenetics, promote angiogenesis, and evade cancer cell survival and apoptosis. HDAC inhibitors could act on cancer cells through multiple mechanisms, primarily by regulating gene expression, inducing cell-cycle arrest, promoting apoptosis, inhibiting angiogenesis, enhancing the immune response, and modifying the epigenome, representing valuable chemical entities for cancer therapy. The benzamide derivatives can chelate with the zinc ion at the active site of HDACs, interact with the surrounding amino acid residues in the active site cavity of HDACs, and cause conformational changes in HDACs. Accordingly, benzamide derivatives are useful HDAC inhibitors, and the benzamide-containing HDAC inhibitors have the potential to demonstrate robust anticancer activity. The purpose of this review is to summarize the current scenario of benzamide-containing HDAC inhibitors with anticancer therapeutic potential developed since 2020 to facilitate further rational exploitation of more effective candidates.
Insights
Benzamide derivatives are potent histone deacetylase (HDAC) inhibitors with anticancer potential. This review highlights recent benzamide-based HDAC inhibitors developed since 2020 for cancer therapy.
Area of Science:
- Medicinal Chemistry
- Molecular Biology
- Oncology
Background:
- Histone deacetylases (HDACs) regulate crucial cellular processes including gene expression, cell cycle, and apoptosis.
- Dysregulation of HDACs is implicated in cancer development and progression.
- HDAC inhibitors represent a promising class of anticancer agents targeting these enzymes.
Purpose of the Study:
- To review benzamide-containing HDAC inhibitors with anticancer potential.
- To summarize novel benzamide-based HDAC inhibitors developed since 2020.
- To guide future development of effective anticancer therapeutics.
Main Methods:
- Literature review of scientific publications and patents.
- Focus on benzamide derivatives targeting HDACs.
- Analysis of anticancer activity and therapeutic potential.
Main Results:
- Benzamide derivatives effectively inhibit HDACs by chelating zinc ions and interacting with active site residues.
- These inhibitors exhibit anticancer activity through multiple mechanisms, including gene expression regulation and apoptosis induction.
- Recent developments showcase promising benzamide-containing HDAC inhibitors for cancer treatment.
Conclusions:
- Benzamide derivatives are valuable HDAC inhibitors with significant anticancer therapeutic potential.
- Continued research into benzamide-based HDAC inhibitors is crucial for developing novel cancer therapies.
- These compounds offer a rational approach for exploiting HDACs in cancer treatment.
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