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Synthesis and biological evaluation of aza-crown ether–squaramide conjugates as anion/cation symporters
Xi-Hui Yu1; Xiong-Jie Cai1; Xiao-Qiao Hong1; Kin Yip Tam2; Kun Zhang3,4; Wen-Hua Chen1
2019-05
Source PublicationFUTURE MEDICINAL CHEMISTRY
ISSN1756-8919
Volume11Issue:10Pages:1091-1106
Abstract

Aim: Anion/cation symport across cellular membranes may lead to cell apoptosis and be developed as a strategy for new anticancer drug discovery. 

Methodology: Four aza-crown ether–squaramide conjugates were synthesized and characterized. Their anion recognition, anion/cation symport, cytotoxicity and probable mechanism of action were investigated in details. 

Conclusion: These conjugates are able to form ion-pairing complexes with chloride anions and facilitate the transmembrane transport of anions via an anion/cation symport process. They can disrupt the cellular homeostasis of chloride anions and sodium cations and induce the basification of acidic organelles in live cells. These conjugates exhibit moderate cytotoxicity toward the tested cancer cells and trigger cell apoptosis by mediating the influx of chloride anions and sodium cations into live cells.

DOI10.4155/fmc-2018-0595
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000478848800002
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Cited Times [WOS]:2   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
Affiliation1.Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, PR China
2.Faculty of Health Sciences, University of Macau, Taipa, Macau, PR China
3.School of Biotechnology & Health Sciences, Wuyi University, Jiangmen 529020, PR China
4.International Healthcare Innovation Institute, Jiangmen 529040, PR China
Recommended Citation
GB/T 7714
Xi-Hui Yu,Xiong-Jie Cai,Xiao-Qiao Hong,et al. Synthesis and biological evaluation of aza-crown ether–squaramide conjugates as anion/cation symporters[J]. FUTURE MEDICINAL CHEMISTRY,2019,11(10):1091-1106.
APA Xi-Hui Yu,Xiong-Jie Cai,Xiao-Qiao Hong,Kin Yip Tam,Kun Zhang,&Wen-Hua Chen.(2019).Synthesis and biological evaluation of aza-crown ether–squaramide conjugates as anion/cation symporters.FUTURE MEDICINAL CHEMISTRY,11(10),1091-1106.
MLA Xi-Hui Yu,et al."Synthesis and biological evaluation of aza-crown ether–squaramide conjugates as anion/cation symporters".FUTURE MEDICINAL CHEMISTRY 11.10(2019):1091-1106.
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