Selective histone deacetylase small molecule inhibitors: recent progress and perspectives

Area of Science:

• Medicinal Chemistry
• Pharmacology
• Drug Discovery

Background:

• Histone deacetylases (HDACs) are crucial in human diseases like cancer and neurodegeneration.
• Aberrant HDAC activity is linked to various pathological conditions.
• The development of isoform- or class-selective HDAC inhibitors is a key area of research.

Purpose of the Study:

• To review recent patents and articles on isoform- or class-selective HDAC inhibitors.
• To discuss the therapeutic potential of these selective inhibitors.
• To highlight advances in drug discovery for HDAC-related diseases.

Main Methods:

• Literature review of patents and research articles from 2012 to present.
• Analysis of structural biology and homology models.
• Identification of novel HDAC inhibitor scaffolds and their modifications.

Main Results:

• Significant progress in developing isoform- or class-selective HDAC inhibitors.
• Identification of hydroxamic acids and benzamides with diverse capping groups.
• Demonstration of potential to circumvent drug toxicity and side effects.

Conclusions:

• HDACs are promising therapeutic targets, especially for cancer.
• Selective HDAC inhibitors offer a promising strategy for disease treatment.
• These inhibitors serve as valuable chemical probes for biological research.