Title:Discovery and Development of HDAC Inhibitors: Approaches for the
Treatment of Cancer a Mini-review
Volume: 21
Issue: 6
Author(s): Roshani Patel*, Arjun Modi and Hitesh Vekariya
Affiliation:
- Department of Pharmaceutical Chemistry, R K University, Rajkot, 360020, Gujarat, India
Keywords:
Histone deacetylase inhibitors, IC50 (μM), cancer cells, acetylation, DNA, transcriptional machinery.
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.
