Preprint Review Version 1 Preserved in Portico This version is not peer-reviewed

SAHA Analogues Bearing Azaheterocycles in CAP Group and Variable Methylene Chain Length: Synthesis and HDAC Inhibitory Ability

Version 1 : Received: 21 November 2023 / Approved: 22 November 2023 / Online: 22 November 2023 (12:20:07 CET)

A peer-reviewed article of this Preprint also exists.

Micheletti, G.; Boga, C.; Drius, G.; Bordoni, S.; Calonghi, N. Suberoylanilide Hydroxamic Acid Analogs with Heteroaryl Amide Group and Different Chain Length: Synthesis and Effect on Histone Deacetylase. Molecules 2024, 29, 238. Micheletti, G.; Boga, C.; Drius, G.; Bordoni, S.; Calonghi, N. Suberoylanilide Hydroxamic Acid Analogs with Heteroaryl Amide Group and Different Chain Length: Synthesis and Effect on Histone Deacetylase. Molecules 2024, 29, 238.

Abstract

This review covers the last 25 years literature on analogs of suberoylanilide hydroxamic acid (SAHA, known also as Vorinostat) acting as 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synthesis and biological activity of compounds where the phenyl group (the surface recognition moiety, CAP) of SAHA has been replaced by an azaheterocycle through a direct bond with amide nitrogen atom, and the methylene chain in the linker region is of variable length.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 reported displayed good to excellent inhibitory activity against HDACs and in many cases showed anti-proliferative activity against human cancer cell lines.

Keywords

HDAC; SAHA; azaheterocycles; synthesis; anticancer

Subject

Biology and Life Sciences, Biochemistry and Molecular Biology

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