Design, synthesis and anticancer evaluation of some novel 7-hydroxy-4-methyl-3-substituted benzopyran-2-one derivatives
Aim: 22 derivatives of 7-hydroxy-4-methyl-3-substituted benzopyran-2-one were designed, synthesized and evaluated for their anticancer activity. Materials & methods: The prepared compounds were screened for their cytotoxicity against the MCF-7 breast cancer cell line. The best five were then evaluated against MCF10a to check their safety and then tested for their PI3K and Akt-1 inhibitory action. The best two derivatives were further analyzed through cell cycle analysis, caspase 3/7 activation, increasing BAX level and decreasing BCL-2. Docking and absorption, distribution, metabolism and excretion prediction studies were also performed. Results & conclusion: Compounds 3b, 3c, 3j, 7 and 8 were the most active. Compounds 3c and 8 showed remarkable inhibitory action against PI3K and Akt-1 enzymes, and both are promising candidates for treatment of breast cancer.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:16 |
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| Enthalten in: |
Future medicinal chemistry - 16(2024), 5 vom: 02. Feb., Seite 417-437 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Abd El-Haleem, Akram H [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 27.02.2024 Date Revised 27.02.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2023-0294 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM368431002 |
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| 100 | 1 | |a Abd El-Haleem, Akram H |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Design, synthesis and anticancer evaluation of some novel 7-hydroxy-4-methyl-3-substituted benzopyran-2-one derivatives |
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| 500 | |a Date Completed 27.02.2024 | ||
| 500 | |a Date Revised 27.02.2024 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Aim: 22 derivatives of 7-hydroxy-4-methyl-3-substituted benzopyran-2-one were designed, synthesized and evaluated for their anticancer activity. Materials & methods: The prepared compounds were screened for their cytotoxicity against the MCF-7 breast cancer cell line. The best five were then evaluated against MCF10a to check their safety and then tested for their PI3K and Akt-1 inhibitory action. The best two derivatives were further analyzed through cell cycle analysis, caspase 3/7 activation, increasing BAX level and decreasing BCL-2. Docking and absorption, distribution, metabolism and excretion prediction studies were also performed. Results & conclusion: Compounds 3b, 3c, 3j, 7 and 8 were the most active. Compounds 3c and 8 showed remarkable inhibitory action against PI3K and Akt-1 enzymes, and both are promising candidates for treatment of breast cancer | ||
| 650 | 4 | |a Journal Article | |
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| 650 | 4 | |a anticancer activity | |
| 650 | 4 | |a benzopyran-2-one | |
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| 700 | 1 | |a Abbas, Safinaz E-S |e verfasserin |4 aut | |
| 700 | 1 | |a El-Ashrey, Mohamed K |e verfasserin |4 aut | |
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