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Current Drug Discovery Technologies

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ISSN (Print): 1570-1638
ISSN (Online): 1875-6220

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Review Article

Discovery and Development of HDAC Inhibitors: Approaches for the Treatment of Cancer a Mini-review

Author(s): Roshani Patel*, Arjun Modi and Hitesh Vekariya

Volume 21, Issue 6, 2024

Published on: 23 February, 2024

Article ID: e230224227378 Pages: 16

DOI: 10.2174/0115701638286941240217102948

Price: $65

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Abstract

Histone deacetylase (HDAC) inhibitors have emerged as promising cancer therapeutics due to their ability to induce differentiation, cell cycle arrest, and apoptosis in cancer cells. In the present review, we have described the systemic discovery and development of HDAC inhibitors. Researchers across the globe have identified various small molecules like benzo[d][1,3]dioxol derivatives, belinostat analogs, pyrazine derivatives, quinazolin-4-one-based derivatives, 2,4-imidazolinedione derivatives, acridine hydroxamic acid derivatives, coumarin derivatives, tetrahydroisoquinoline derivatives, thiazole-5-carboxamide, salicylamide derivatives, β-peptoid-capped HDAC inhibitors, quinazoline derivatives, benzimidazole and benzothiazole derivatives, and β- elemene scaffold containing HDAC inhibitors. Most of the scaffolds have shown attractive IC50 (μM) in various cell lines like HDAC1, HDAC2, HDAC6, PI3K, HeLa, MDA-MB-231, MCF-10A, MCF-7, U937, K562 and Bcr-Abl cell lines.

Keywords: Histone deacetylase inhibitors, IC50 (μM), cancer cells, acetylation, DNA, transcriptional machinery.

Graphical Abstract

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