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Updated: Feb 16, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Novel Polyamine-Naphthalene Diimide Conjugates Targeting Histone Deacetylases and DNA for Cancer Phenotype
Alice Pasini1, Chiara Marchetti2, Claudia Sissi3
1Department of Electrical, Electronic and Information Engineering "Guglielmo Marconi" (DEI), Alma Mater Studiorum-University of Bologna, Via Venezia 52, 47521 Cesena (FC), Italy.
Abstract:
A series of hybrid compounds was designed to target histone deacetylases and ds-/G-quadruplex DNAs by merging structural features deriving from Scriptaid and compound 1. Compound 6 binds different DNA arrangements, inhibits HDACs both in vitro and in cells, and is able to induce a reduction of cell proliferation. Moreover, compound 6 displays cell phenotype-reprogramming properties since it prevents the epithelial to mesenchymal transition in cancer cells, inducing a less aggressive and migratory phenotype, which is one of the goals of present innovative strategies in cancer therapies.
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