Synthesis of potent and selective HDAC6 inhibitors led to unexpected opening of a quinazoline ring-Reference-Cited by-同舟云学术

Synthesis of potent and selective HDAC6 inhibitors led to unexpected opening of a quinazoline ring

Published:2022 Issue:18 Volume:12 Page:11548-11556
ISSN:2046-2069
Container-title:RSC Advances
language:en
Short-container-title:RSC Adv.

Author:

Moi Davide¹²,Citarella Andrea¹²,Bonanni Davide¹,Pinzi Luca¹,Passarella Daniele²^ORCID,Silvani Alessandra²^ORCID,Giannini Clelia²^ORCID,Rastelli Giulio¹^ORCID

Affiliation:

1. Department of Life Sciences, University of Modena and Reggio Emilia, Via Campi 103, Modena 41125, Italy

2. Department of Chemistry, University of Milan, Via Golgi 19, Milano 20133, Italy

Abstract

Potent and selective inhibitors of HDAC6 have been designed, synthesized and tested. An unexpected opening of the quinazoline ring led to both aminotriazoloquinazoline and aminotriazole compounds with potent activity and isoform selectivity.

Funder

Associazione Italiana per la Ricerca sul Cancro

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemical Engineering,General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2022/RA/D2RA01753A

Reference36 articles.

1. Epigenetic regulation of gene expression: how the genome integrates intrinsic and environmental signals

2. Dual Targeting Strategies On Histone Deacetylase 6 (HDAC6) And Heat Shock Protein 90 (Hsp90)

3. Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight