Development of novel benzamide class I selective lysine deacetylase inhibitors as potent anticancer agents

• Published in: Journal of enzyme inhibition and medicinal chemistry Vol. 40; no. 1; p. 2520612
• Main Authors: Gill, Jason H., Sellars, Jonathan D., Waddell, Paul G., Shnyder, Steven D., Grigg, Ronald, Fishwick, Colin W. G.
• Format: Journal Article
• Language: English
• Published: England Taylor & Francis 01.12.2025; Taylor & Francis Group
• Subjects: aminobenzamide; Animals; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Benzamides - chemical synthesis; Benzamides - chemistry; Benzamides - pharmacology; cancer chemotherapy; Cell Line, Tumor; Cell Proliferation - drug effects; Dose-Response Relationship, Drug; Drug Development; Drug Screening Assays, Antitumor; Female; HDAC Inhibitor; histone deacetylase (HDACs); Histone Deacetylase Inhibitors - chemical synthesis; Histone Deacetylase Inhibitors - chemistry; Histone Deacetylase Inhibitors - pharmacology; Histone Deacetylases - metabolism; Humans; Lysine Deacetylase (KDACs); Mice; Molecular Structure; protein acetylation; Structure-Activity Relationship; benzamide; Lysine Deacetylase (KDACs); cancer chemotherapy; protein acetylation; HDAC Inhibitor; histone deacetylase (HDACs); aminobenzamide

Small molecule inhibitors of lysine deacetylases (KDACs), exemplified by histone deacetylases (HDACs), exhibit significant promise as cancer therapeutics. Using a modular combinatorial chemistry approach, a novel class of KDAC inhibitors (KDACi) containing the aminophenyl-benzamide headgroup have be...