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Molecules 2018, 23(6), 1396; https://doi.org/10.3390/molecules23061396

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

Department of Medicinal Chemistry, School of Pharmacy, Fudan University, No. 826, Zhangheng Rd., Shanghai 201203, China
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Received: 13 May 2018 / Revised: 1 June 2018 / Accepted: 4 June 2018 / Published: 8 June 2018
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Abstract

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. View Full-Text
Keywords: phosphoglycerate mutase 1; inhibitors; anti-cancer; xanthone phosphoglycerate mutase 1; inhibitors; anti-cancer; xanthone
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Wang, P.; Jiang, L.; Cao, Y.; Ye, D.; Zhou, L. The Design and Synthesis of N-Xanthone Benzenesulfonamides as Novel Phosphoglycerate Mutase 1 (PGAM1) Inhibitors. Molecules 2018, 23, 1396.

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