Design, synthesis and anti-cervical cancer activity of aroylpyrrole-based derivatives as potent histone deacetylase 6 inhibitors.

ABSTRACT: Cancers, such as cervical carcinoma, are one of the most significant diseases affecting human health and histone deacetylases (HDACs) are striking targets in current antitumor drug development. Compared to pan-HDAC inhibitors with potential toxicity, the development of selective HDAC6 inhibitors (sHDAC6is) is a major research focus. In this study, a series of derivatives bearing an aroylpyrrole core were designed and synthesized using a scaffold-hopping strategy. Among these, the best compound 4-benzoyl-1-(4-fluorobenzyl)-N-(7-(hydroxyamino)-7-oxoheptyl)-1H-pyrrole-2-carboxamide (10g) inhibited HDAC6 with an IC₅₀ of 3.9 nM and superior selectivity over HDAC1 compared to ACY-1215. In vitro, these aroylpyrroles demonstrated promising antiproliferative activiti

SUBMITTER: Wang X 

PROVIDER: S-EPMC12679430 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature