Ring size changes in the development of class I HDAC inhibitors

Five pathways involving different ring structures led to generation of fourteen thienylbenzamides (7–20) which display the structure-activity relationships of class I HDAC inhibitors. All the synthesised compounds inhibit HDAC1 and HDAC2 selectively over other isoforms and many inhibit DLD1 and HCT1...

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Autores principales: Cho, Er-Chieh, Liu, Chi-Yuan, Tang, Di-Wei, Lee, Hsueh-Yun
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2021
Materias:
Research Paper
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8231390/
https://www.ncbi.nlm.nih.gov/pubmed/34167419
http://dx.doi.org/10.1080/14756366.2021.1941920
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author Cho, Er-Chieh
Liu, Chi-Yuan
Tang, Di-Wei
Lee, Hsueh-Yun
author_facet Cho, Er-Chieh
Liu, Chi-Yuan
Tang, Di-Wei
Lee, Hsueh-Yun
author_sort Cho, Er-Chieh
collection PubMed
description Five pathways involving different ring structures led to generation of fourteen thienylbenzamides (7–20) which display the structure-activity relationships of class I HDAC inhibitors. All the synthesised compounds inhibit HDAC1 and HDAC2 selectively over other isoforms and many inhibit DLD1 and HCT116 cells more effectively than a parent compound. Compounds 8 and 16 inhibit HCT116 cells by activation of the apoptosis pathway.
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spelling pubmed-82313902021-07-01 Ring size changes in the development of class I HDAC inhibitors Cho, Er-Chieh Liu, Chi-Yuan Tang, Di-Wei Lee, Hsueh-Yun J Enzyme Inhib Med Chem Research Paper Five pathways involving different ring structures led to generation of fourteen thienylbenzamides (7–20) which display the structure-activity relationships of class I HDAC inhibitors. All the synthesised compounds inhibit HDAC1 and HDAC2 selectively over other isoforms and many inhibit DLD1 and HCT116 cells more effectively than a parent compound. Compounds 8 and 16 inhibit HCT116 cells by activation of the apoptosis pathway. Taylor & Francis 2021-06-24 /pmc/articles/PMC8231390/ /pubmed/34167419 http://dx.doi.org/10.1080/14756366.2021.1941920 Text en © 2021 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Paper
Cho, Er-Chieh
Liu, Chi-Yuan
Tang, Di-Wei
Lee, Hsueh-Yun
Ring size changes in the development of class I HDAC inhibitors
title Ring size changes in the development of class I HDAC inhibitors
title_full Ring size changes in the development of class I HDAC inhibitors
title_fullStr Ring size changes in the development of class I HDAC inhibitors
title_full_unstemmed Ring size changes in the development of class I HDAC inhibitors
title_short Ring size changes in the development of class I HDAC inhibitors
title_sort ring size changes in the development of class i hdac inhibitors
topic Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8231390/
https://www.ncbi.nlm.nih.gov/pubmed/34167419
http://dx.doi.org/10.1080/14756366.2021.1941920
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AT liuchiyuan ringsizechangesinthedevelopmentofclassihdacinhibitors
AT tangdiwei ringsizechangesinthedevelopmentofclassihdacinhibitors
AT leehsuehyun ringsizechangesinthedevelopmentofclassihdacinhibitors

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