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

  • Molecules. 2018 Jun 8;23(6):1396. doi: 10.3390/molecules23061396.
Penghui Wang  1 ,  Lulu Jiang  2 ,  Yang Cao  3 ,  Deyong Ye  4 ,  Lu Zhou  5
Affiliations
  • 1. Department of Medicinal Chemistry, School of Pharmacy, Fudan University, No. 826, Zhangheng Rd., Shanghai 201203, China. [email protected].
  • 2. Department of Medicinal Chemistry, School of Pharmacy, Fudan University, No. 826, Zhangheng Rd., Shanghai 201203, China. [email protected].
  • 3. Department of Medicinal Chemistry, School of Pharmacy, Fudan University, No. 826, Zhangheng Rd., Shanghai 201203, China. [email protected].
  • 4. Department of Medicinal Chemistry, School of Pharmacy, Fudan University, No. 826, Zhangheng Rd., Shanghai 201203, China. [email protected].
  • 5. Department of Medicinal Chemistry, School of Pharmacy, Fudan University, No. 826, Zhangheng Rd., Shanghai 201203, China. [email protected].
PMID: 29890679 DOI: 10.3390/molecules23061396
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.

Keywords
anti-cancer; inhibitors; phosphoglycerate mutase 1; xanthone.
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