Synthesis and biological evaluation of novel imidazopyrimidin-3-amines as anticancer agents
© 2016 John Wiley & Sons A/S..
Groebke-Blackburn-Bienayme reaction has been utilized for the synthesis of new imidazo[1,2-a]pyrimidine derivatives as novel anticancer agents. The cytotoxic activities of compounds were evaluated against human cancer cell lines including MCF-7, T-47D, and MDA-MB-231, compared with etoposide as the standard drug. Among the tested compounds, hydroxy- and/or methoxy-phenyl derivatives (6a-c and 6k) with IC50 values of 6.72-14.36 μm were more potent than etoposide against all cell lines. The acridine orange/ethidium bromide double staining and DNA fragmentation studies demonstrated that the cytotoxic effect of 3-hydroxy-4-methoxyphenyl derivative 6c is associated with apoptosis in cancer cells.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2017 |
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| Erschienen: |
2017 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:89 |
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| Enthalten in: |
Chemical biology & drug design - 89(2017), 5 vom: 03. Mai, Seite 797-805 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Mahdavi, Mohammad [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 09.05.2017 Date Revised 12.10.2018 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1111/cbdd.12904 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a Groebke-Blackburn-Bienayme reaction has been utilized for the synthesis of new imidazo[1,2-a]pyrimidine derivatives as novel anticancer agents. The cytotoxic activities of compounds were evaluated against human cancer cell lines including MCF-7, T-47D, and MDA-MB-231, compared with etoposide as the standard drug. Among the tested compounds, hydroxy- and/or methoxy-phenyl derivatives (6a-c and 6k) with IC50 values of 6.72-14.36 μm were more potent than etoposide against all cell lines. The acridine orange/ethidium bromide double staining and DNA fragmentation studies demonstrated that the cytotoxic effect of 3-hydroxy-4-methoxyphenyl derivative 6c is associated with apoptosis in cancer cells | ||
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| 700 | 1 | |a Foroumadi, Alireza |e verfasserin |4 aut | |
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