Synthesis and biological evaluation of aza-crown ether-squaramide conjugates as anion/cation symporters
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.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2019 |
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| Erschienen: |
2019 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:11 |
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| Enthalten in: |
Future medicinal chemistry - 11(2019), 10 vom: 15. Mai, Seite 1091-1106 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Yu, Xi-Hui [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 10.02.2020 Date Revised 10.02.2020 published: Print Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2018-0595 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM298941147 |
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| 245 | 1 | 0 | |a Synthesis and biological evaluation of aza-crown ether-squaramide conjugates as anion/cation symporters |
| 264 | 1 | |c 2019 | |
| 336 | |a Text |b txt |2 rdacontent | ||
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| 500 | |a Date Completed 10.02.2020 | ||
| 500 | |a Date Revised 10.02.2020 | ||
| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a 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 | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a anion/cation symporter | |
| 650 | 4 | |a anionophoric activity | |
| 650 | 4 | |a antiproliferative activity | |
| 650 | 4 | |a aza-crown ether | |
| 650 | 4 | |a squaramide | |
| 650 | 7 | |a Anions |2 NLM | |
| 650 | 7 | |a Antineoplastic Agents |2 NLM | |
| 650 | 7 | |a Aza Compounds |2 NLM | |
| 650 | 7 | |a Cations |2 NLM | |
| 650 | 7 | |a Crown Ethers |2 NLM | |
| 650 | 7 | |a squaramide |2 NLM | |
| 650 | 7 | |a Quinine |2 NLM | |
| 650 | 7 | |a A7V27PHC7A |2 NLM | |
| 700 | 1 | |a Cai, Xiong-Jie |e verfasserin |4 aut | |
| 700 | 1 | |a Hong, Xiao-Qiao |e verfasserin |4 aut | |
| 700 | 1 | |a Tam, Kin Yip |e verfasserin |4 aut | |
| 700 | 1 | |a Zhang, Kun |e verfasserin |4 aut | |
| 700 | 1 | |a Chen, Wen-Hua |e verfasserin |4 aut | |
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| 773 | 1 | 8 | |g volume:11 |g year:2019 |g number:10 |g day:15 |g month:05 |g pages:1091-1106 |
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