Dual activity of indolin-2-ones containing an arylidene motif : DNA and BSA interaction
This journal is © The Royal Society of Chemistry..
Applying a multistep approach, novel indolin-2-ones (IND) that possess an arylidene motif have been synthesized. Eight compounds were chosen for different biological tests (antimicrobial and cytotoxicity). IND containing 2-thienyl (4h) fragment have been found to exhibit good antimicrobial activity against B. cereus. Molecules that have 3-aminophenyl (4d) or 2-pyridyl (4g) groups have shown the best antifungal activities against all tested fungi. These compounds have also been noticed as promising pharmaceuticals against MCF-7 cancer cell lines. Experimental outcomes from the investigation of the interaction of 4d with DNA implied its moderate binding to DNA (KSV = 1.35 × 104 and 3.05 × 104 M-1 for EB and Hoechst binder, respectively). However, considerably stronger binding of 4d to BSA has been evidenced (Ka = 6.1 × 106 M-1). In summary, IND that contains m-aminobenzylidene fragment (4d) exhibits a good dual biological activity making it a promising candidate for further investigation in the drug discovery sector.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:13 |
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| Enthalten in: |
RSC advances - 13(2023), 40 vom: 18. Sept., Seite 28139-28147 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Bukhari, Syed Nasir Abbas [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Revised 28.09.2023 published: Electronic-eCollection Citation Status PubMed-not-MEDLINE |
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| doi: |
10.1039/d3ra04997c |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM362497214 |
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| 500 | |a published: Electronic-eCollection | ||
| 500 | |a Citation Status PubMed-not-MEDLINE | ||
| 520 | |a This journal is © The Royal Society of Chemistry. | ||
| 520 | |a Applying a multistep approach, novel indolin-2-ones (IND) that possess an arylidene motif have been synthesized. Eight compounds were chosen for different biological tests (antimicrobial and cytotoxicity). IND containing 2-thienyl (4h) fragment have been found to exhibit good antimicrobial activity against B. cereus. Molecules that have 3-aminophenyl (4d) or 2-pyridyl (4g) groups have shown the best antifungal activities against all tested fungi. These compounds have also been noticed as promising pharmaceuticals against MCF-7 cancer cell lines. Experimental outcomes from the investigation of the interaction of 4d with DNA implied its moderate binding to DNA (KSV = 1.35 × 104 and 3.05 × 104 M-1 for EB and Hoechst binder, respectively). However, considerably stronger binding of 4d to BSA has been evidenced (Ka = 6.1 × 106 M-1). In summary, IND that contains m-aminobenzylidene fragment (4d) exhibits a good dual biological activity making it a promising candidate for further investigation in the drug discovery sector | ||
| 650 | 4 | |a Journal Article | |
| 700 | 1 | |a Alsahli, Tariq G |e verfasserin |4 aut | |
| 700 | 1 | |a Ejaz, Hasan |e verfasserin |4 aut | |
| 700 | 1 | |a Ahmed, Naveed |e verfasserin |4 aut | |
| 700 | 1 | |a Ahmad, Waqas |e verfasserin |4 aut | |
| 700 | 1 | |a Elsherif, Mervat A |e verfasserin |4 aut | |
| 700 | 1 | |a Alotaibi, Nasser H |e verfasserin |4 aut | |
| 700 | 1 | |a Junaid, Kashaf |e verfasserin |4 aut | |
| 700 | 1 | |a Janković, Nenad |e verfasserin |4 aut | |
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