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Updated: Jul 5, 2025

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Suberoylanilide Hydroxamic Acid Analogs with Heteroaryl Amide Group and Different Chain Length: Synthesis and Effect
Gabriele Micheletti1, Carla Boga1, Giacomo Drius1
1Department of Industrial Chemistry 'Toso Montanari', Alma Mater Studiorum, Università di Bologna, Viale Del Risorgimento 4, 40136 Bologna, Italy.
Abstract:
This review covers the last 25 years of the literature on analogs of suberoylanilide hydroxamic acid (SAHA, known also as vorinostat) acting as an HDAC inhibitor. In particular, the topic has been focused on the synthesis and biological activity of compounds where the phenyl group (the surface recognition moiety, CAP) of SAHA has been replaced by an azaheterocycle through a direct bond with amide nitrogen atom, and the methylene chain in the linker region is of variable length. Most of the compounds displayed good to excellent inhibitory activity against HDACs and in many cases showed antiproliferative activity against human cancer cell lines.
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