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ORIGINAL RESEARCH article
Front. Chem.
Sec. Organic Chemistry
Volume 12 - 2024 |
doi: 10.3389/fchem.2024.1529211
This article is part of the Research Topic Recent Advances in Synthetic Organic Chemistry at the Biomedical Interface: Honoring Professor Iwao Ojima on the Occasion of his 80th Birthday View all articles
Design and synthesis of phenylthiophosphoryl dichloride derivatives and evaluation of their antitumour and anti-inflammatory activities
Provisionally accepted- Qinhuangdao Maternal and Child Health Hospital, Qinhuangdao, China
Tumours and inflammation are serious risks to human health and are importantly regulated by the gas signalling molecule hydrogen sulphide. In this work, we report the rational design and synthesis of H2S donor molecules based on phenylthiophosphoryl dichloride nuclei and assess their efficacy against tumours and inflammation. We predicted its potential anticancer targets based on network pharmacology and then verified the inhibitory effect of the active compound S11 on the pathway PI3K/AKT by enzyme inhibition and molecular docking assay. In addition, compound S11 exhibited a potent antiinflammatory effect on macrophages, effectively reducing the levels of inflammatory mediators TNF-α, IL-10 and HO-1. Compound S11 can be used as a new chemical entity for the discovery of new anti-cancer drugs or antiinflammatory drugs.
Keywords: Hydrogen Sulfide, Network Pharmacology, anti-tumor, anti-inflammatory, phenylthiophosphoryl dichloride
Received: 16 Nov 2024; Accepted: 24 Dec 2024.
Copyright: © 2024 Xu, Yang, Yu and Wang. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
* Correspondence:
Chunyun Xu, Qinhuangdao Maternal and Child Health Hospital, Qinhuangdao, China
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