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synthesis and biological activity of compounds where the phenyl group (the surface recognition moiety, CAP) of SAHA has been replaced by an azaheterocycle through a direct bond with amide nitrogen atom, and the methylene chain in the linker region is of variable length.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.

Suberoylanilide Hydroxamic Acid Analogs with Heteroaryl Amide Group and Different Chain Length: Synthesis and Effect on Histone Deacetylase / GABRIELE MICHELETTI; Boga Carla; Giacomo Drius; silvia bordoni; Natalia Calonghi. - In: MOLECULES. - ISSN 1420-3049. - ELETTRONICO. - 29:1(2024), pp. 238.1-238.23. [10.3390/molecules29010238]

Suberoylanilide Hydroxamic Acid Analogs with Heteroaryl Amide Group and Different Chain Length: Synthesis and Effect on Histone Deacetylase

GABRIELE MICHELETTI
Primo
Membro del Collaboration Group
;
Boga Carla
Conceptualization
;
Giacomo Drius
Membro del Collaboration Group
;
silvia bordoni
Penultimo
Membro del Collaboration Group
;
Natalia Calonghi
Ultimo
Membro del Collaboration Group
2024

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synthesis and biological activity of compounds where the phenyl group (the surface recognition moiety, CAP) of SAHA has been replaced by an azaheterocycle through a direct bond with amide nitrogen atom, and the methylene chain in the linker region is of variable length.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.
2024
Suberoylanilide Hydroxamic Acid Analogs with Heteroaryl Amide Group and Different Chain Length: Synthesis and Effect on Histone Deacetylase / GABRIELE MICHELETTI; Boga Carla; Giacomo Drius; silvia bordoni; Natalia Calonghi. - In: MOLECULES. - ISSN 1420-3049. - ELETTRONICO. - 29:1(2024), pp. 238.1-238.23. [10.3390/molecules29010238]
GABRIELE MICHELETTI; Boga Carla; Giacomo Drius; silvia bordoni; Natalia Calonghi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11585/955188
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