Synthesis and anticancer activity of open-resorcinarene conjugates
Copyright © 2020 Elsevier Ltd. All rights reserved..
The first example of conjugation of open-resorcinarenes with chlorambucil, ibuprofen, naproxen and indomethacin are presented. The cytotoxic properties of the obtained conjugates were tested against the cancer cell lines U-251, PC-3, K-562, HCT-15, MCF-7 and SKLU-1. It was found that the conjugate with chlorambucil, naproxen or indomethacin (having 8 moieties) was toxic towards cancer cell lines U-251 and K-562, with no activity against non-cancerous COS-7 cells. The conjugates with naproxen and indomethacin showed high selectivity towards U-251 tumor cells.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:30 |
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| Enthalten in: |
Bioorganic & medicinal chemistry letters - 30(2020), 14 vom: 15. Juli, Seite 127275 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Daniel Pedro-Hernández, Luis [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 01.06.2021 Date Revised 01.06.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.bmcl.2020.127275 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM311067530 |
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| 500 | |a published: Print-Electronic | ||
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| 520 | |a Copyright © 2020 Elsevier Ltd. All rights reserved. | ||
| 520 | |a The first example of conjugation of open-resorcinarenes with chlorambucil, ibuprofen, naproxen and indomethacin are presented. The cytotoxic properties of the obtained conjugates were tested against the cancer cell lines U-251, PC-3, K-562, HCT-15, MCF-7 and SKLU-1. It was found that the conjugate with chlorambucil, naproxen or indomethacin (having 8 moieties) was toxic towards cancer cell lines U-251 and K-562, with no activity against non-cancerous COS-7 cells. The conjugates with naproxen and indomethacin showed high selectivity towards U-251 tumor cells | ||
| 650 | 4 | |a Journal Article | |
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| 650 | 4 | |a Anticancer activity | |
| 650 | 4 | |a Chlorambucil | |
| 650 | 4 | |a Dendrimers | |
| 650 | 4 | |a Nonsteroidal anti-inflammatory drugs | |
| 650 | 4 | |a Open-resorcinarene | |
| 650 | 7 | |a Antineoplastic Agents |2 NLM | |
| 650 | 7 | |a resorcinarene |2 NLM | |
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| 700 | 1 | |a Martínez-Klimova, Elena |e verfasserin |4 aut | |
| 700 | 1 | |a Ramírez-Ápan, Teresa |e verfasserin |4 aut | |
| 700 | 1 | |a Martínez-García, Marcos |e verfasserin |4 aut | |
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