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

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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Main Authors: Penghui Wang, Lulu Jiang, Yang Cao, Deyong Ye, Lu Zhou
Format: Article
Language:English
Published: MDPI AG 2018-06-01
Series:Molecules
Subjects:
phosphoglycerate mutase 1
inhibitors
anti-cancer
xanthone
Online Access:http://www.mdpi.com/1420-3049/23/6/1396
id doaj-5bd1d3af2da449d191030a9ff6ea2df6
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spelling doaj-5bd1d3af2da449d191030a9ff6ea2df62020-11-25T02:26:56ZengMDPI AGMolecules1420-30492018-06-01236139610.3390/molecules23061396molecules23061396The Design and Synthesis of N-Xanthone Benzenesulfonamides as Novel Phosphoglycerate Mutase 1 (PGAM1) InhibitorsPenghui Wang0Lulu Jiang1Yang Cao2Deyong Ye3Lu Zhou4Department of Medicinal Chemistry, School of Pharmacy, Fudan University, No. 826, Zhangheng Rd., Shanghai 201203, ChinaDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, No. 826, Zhangheng Rd., Shanghai 201203, ChinaDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, No. 826, Zhangheng Rd., Shanghai 201203, ChinaDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, No. 826, Zhangheng Rd., Shanghai 201203, ChinaDepartment of Medicinal Chemistry, School of Pharmacy, Fudan University, No. 826, Zhangheng Rd., Shanghai 201203, ChinaUpregulation 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 IC50 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.http://www.mdpi.com/1420-3049/23/6/1396phosphoglycerate mutase 1inhibitorsanti-cancerxanthone
collection DOAJ
language English
format Article
sources DOAJ
author Penghui Wang
Lulu Jiang
Yang Cao
Deyong Ye
Lu Zhou
spellingShingle Penghui Wang
Lulu Jiang
Yang Cao
Deyong Ye
Lu Zhou
The Design and Synthesis of N-Xanthone Benzenesulfonamides as Novel Phosphoglycerate Mutase 1 (PGAM1) Inhibitors
Molecules
phosphoglycerate mutase 1
inhibitors
anti-cancer
xanthone
author_facet Penghui Wang
Lulu Jiang
Yang Cao
Deyong Ye
Lu Zhou
author_sort Penghui Wang
title 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_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_sort design and synthesis of n-xanthone benzenesulfonamides as novel phosphoglycerate mutase 1 (pgam1) inhibitors
publisher MDPI AG
series Molecules
issn 1420-3049
publishDate 2018-06-01
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 IC50 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.
topic phosphoglycerate mutase 1
inhibitors
anti-cancer
xanthone
url http://www.mdpi.com/1420-3049/23/6/1396
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