Cytotoxic Activity of Unique Synthesized Five-membered Heterocyclic Compounds Coordinated with Tiopronin Monovalent
Copyright© Bentham Science Publishers; For any queries, please email at epubbenthamscience.net..
BACKGROUND: We recently synthesized a compound in which 5-mercapto-1-methyltetrazole (MM4) was coordinated to tiopronin monovalent (TPN-Au(I)) and reported its cytotoxic activity against human leukemia cells in vitro</i>.
OBJECTIVE: We further synthesized other heterocyclic compounds coordinated with TPN-Au(I) and assessed their cytotoxic activity against hepatocellular carcinoma HepG2 and lung cancer cell line H1299 in vitro</i>.
METHODS: Seven kinds of compounds were synthesized by introducing a five-membered heterocyclic compound into TPN-Au(I). The number of viable cells was counted by a trypan blue dye exclusion assay. Fluorescence conjugated-Annexin V and propidium iodide were used for the apoptosis analysis.
RESULTS: Seven compounds were successfully synthesized. Among these compounds, TPN-Au(I)-MTZ (3- mercapto-1,2,4-triazole), TPN-Au(I)-MMT (2-mercapto-5-methyl-1,3,4-thiadiazole), and TPN-Au(I)-MMTT (2-mercapto-5-methylthio-1,3,4-thiadiazole) effectively suppressed the proliferation and induced apoptosis in HepG2 cells. In addition, TPN-Au(I)-MMTT and TPN-Au(I)-MMT also showed effective cytotoxicity against H1299 cells.
CONCLUSION: The present results showed that introduction of some five-membered heterocyclic compounds, especially MMT and MMTT, to TPN-Au(I) improved the cytotoxicity against solid cancer cells.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:29 |
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| Enthalten in: |
Current pharmaceutical design - 29(2023), 12 vom: 07., Seite 957-965 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Sano, Naoyuki [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 29.05.2023 Date Revised 03.06.2023 published: Print Citation Status MEDLINE |
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| doi: |
10.2174/1381612829666230407094658 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM355371421 |
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| 100 | 1 | |a Sano, Naoyuki |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Cytotoxic Activity of Unique Synthesized Five-membered Heterocyclic Compounds Coordinated with Tiopronin Monovalent |
| 264 | 1 | |c 2023 | |
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| 500 | |a Date Completed 29.05.2023 | ||
| 500 | |a Date Revised 03.06.2023 | ||
| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright© Bentham Science Publishers; For any queries, please email at epubbenthamscience.net. | ||
| 520 | |a BACKGROUND: We recently synthesized a compound in which 5-mercapto-1-methyltetrazole (MM4) was coordinated to tiopronin monovalent (TPN-Au(I)) and reported its cytotoxic activity against human leukemia cells in vitro</i> | ||
| 520 | |a OBJECTIVE: We further synthesized other heterocyclic compounds coordinated with TPN-Au(I) and assessed their cytotoxic activity against hepatocellular carcinoma HepG2 and lung cancer cell line H1299 in vitro</i> | ||
| 520 | |a METHODS: Seven kinds of compounds were synthesized by introducing a five-membered heterocyclic compound into TPN-Au(I). The number of viable cells was counted by a trypan blue dye exclusion assay. Fluorescence conjugated-Annexin V and propidium iodide were used for the apoptosis analysis | ||
| 520 | |a RESULTS: Seven compounds were successfully synthesized. Among these compounds, TPN-Au(I)-MTZ (3- mercapto-1,2,4-triazole), TPN-Au(I)-MMT (2-mercapto-5-methyl-1,3,4-thiadiazole), and TPN-Au(I)-MMTT (2-mercapto-5-methylthio-1,3,4-thiadiazole) effectively suppressed the proliferation and induced apoptosis in HepG2 cells. In addition, TPN-Au(I)-MMTT and TPN-Au(I)-MMT also showed effective cytotoxicity against H1299 cells | ||
| 520 | |a CONCLUSION: The present results showed that introduction of some five-membered heterocyclic compounds, especially MMT and MMTT, to TPN-Au(I) improved the cytotoxicity against solid cancer cells | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a 2 | |
| 650 | 4 | |a 2-mercapto-5- methyl-1 | |
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| 650 | 4 | |a 4-thiadiazole (MMT) | |
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| 650 | 4 | |a 4-triazole (MTZ) | |
| 650 | 4 | |a 5-membered heterocyclic compound | |
| 650 | 4 | |a Tiopronin monovalent (TPN-Au(I)) | |
| 650 | 4 | |a cytotoxicity | |
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| 650 | 7 | |a Antineoplastic Agents |2 NLM | |
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| 700 | 1 | |a Yoshino, Hironori |e verfasserin |4 aut | |
| 700 | 1 | |a Sato, Yoshiaki |e verfasserin |4 aut | |
| 700 | 1 | |a Honma, Hideo |e verfasserin |4 aut | |
| 700 | 1 | |a Cordonier, Christopher E J |e verfasserin |4 aut | |
| 700 | 1 | |a Kashiwakura, Ikuo |e verfasserin |4 aut | |
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