The Design and Synthesis of N-Xanthone Benzenesulfonamides as Novel Phosphoglycerate Mutase 1 (PGAM1) Inhibitors

Upregulation of phosphoglycerate mutase 1 (PGAM1) has been identified as one common phenomenon in a variety of cancers. Inhibition of PGAM1 provides a new promising therapeutic strategy for cancer treatment. Herein, based on our previous work, a series of new N-xanthone benzenesulfonamides were disc...

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Detalles Bibliográficos
Autores principales: Wang, Penghui, Jiang, Lulu, Cao, Yang, Ye, Deyong, Zhou, Lu
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6100356/
https://www.ncbi.nlm.nih.gov/pubmed/29890679
http://dx.doi.org/10.3390/molecules23061396
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author Wang, Penghui
Jiang, Lulu
Cao, Yang
Ye, Deyong
Zhou, Lu
author_facet Wang, Penghui
Jiang, Lulu
Cao, Yang
Ye, Deyong
Zhou, Lu
author_sort Wang, Penghui
collection PubMed
description Upregulation of phosphoglycerate mutase 1 (PGAM1) has been identified as one common phenomenon in a variety of cancers. Inhibition of PGAM1 provides a new promising therapeutic strategy for cancer treatment. Herein, based on our previous work, a series of new N-xanthone benzenesulfonamides were discovered as novel PGAM1 inhibitors. The representative molecule 15h, with an IC(50) of 2.1 μM, showed an enhanced PGAM1 inhibitory activity and higher enzyme inhibitory specificity compared to PGMI-004A, as well as a slightly improved antiproliferative activity.
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spelling pubmed-61003562018-11-13 The Design and Synthesis of N-Xanthone Benzenesulfonamides as Novel Phosphoglycerate Mutase 1 (PGAM1) Inhibitors Wang, Penghui Jiang, Lulu Cao, Yang Ye, Deyong Zhou, Lu Molecules Communication Upregulation of phosphoglycerate mutase 1 (PGAM1) has been identified as one common phenomenon in a variety of cancers. Inhibition of PGAM1 provides a new promising therapeutic strategy for cancer treatment. Herein, based on our previous work, a series of new N-xanthone benzenesulfonamides were discovered as novel PGAM1 inhibitors. The representative molecule 15h, with an IC(50) of 2.1 μM, showed an enhanced PGAM1 inhibitory activity and higher enzyme inhibitory specificity compared to PGMI-004A, as well as a slightly improved antiproliferative activity. MDPI 2018-06-08 /pmc/articles/PMC6100356/ /pubmed/29890679 http://dx.doi.org/10.3390/molecules23061396 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Communication
Wang, Penghui
Jiang, Lulu
Cao, Yang
Ye, Deyong
Zhou, Lu
The Design and Synthesis of N-Xanthone Benzenesulfonamides as Novel Phosphoglycerate Mutase 1 (PGAM1) Inhibitors
title The Design and Synthesis of N-Xanthone Benzenesulfonamides as Novel Phosphoglycerate Mutase 1 (PGAM1) Inhibitors
title_full The Design and Synthesis of N-Xanthone Benzenesulfonamides as Novel Phosphoglycerate Mutase 1 (PGAM1) Inhibitors
title_fullStr The Design and Synthesis of N-Xanthone Benzenesulfonamides as Novel Phosphoglycerate Mutase 1 (PGAM1) Inhibitors
title_full_unstemmed The Design and Synthesis of N-Xanthone Benzenesulfonamides as Novel Phosphoglycerate Mutase 1 (PGAM1) Inhibitors
title_short The Design and Synthesis of N-Xanthone Benzenesulfonamides as Novel Phosphoglycerate Mutase 1 (PGAM1) Inhibitors
title_sort design and synthesis of n-xanthone benzenesulfonamides as novel phosphoglycerate mutase 1 (pgam1) inhibitors
topic Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6100356/
https://www.ncbi.nlm.nih.gov/pubmed/29890679
http://dx.doi.org/10.3390/molecules23061396
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