Design, synthesis and evaluation of novel 2,2-dimethyl-2,3-dihydroquinolin-4(1H)-one based chalcones as cytotoxic agents
We designed and synthesised a series of novel chalcones, incorporating the heterocyclic framework of 2,2-dimethyl-2,3-dihydro-4(1H)-quinolinone, which was prepared via Sonogashira coupling of a substituted orthoaniline under aqueous conditions using Pd catalysis followed by acid-mediated cyclisation...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2018-09-01
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| Series: | Heliyon |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S2405844018327129 |
| _version_ | 1818030137900269568 |
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| author | Julie Jean David S. Farrell Angela M. Farrelly Sinead Toomey James W. Barlow |
| author_facet | Julie Jean David S. Farrell Angela M. Farrelly Sinead Toomey James W. Barlow |
| author_sort | Julie Jean |
| collection | DOAJ |
| description | We designed and synthesised a series of novel chalcones, incorporating the heterocyclic framework of 2,2-dimethyl-2,3-dihydro-4(1H)-quinolinone, which was prepared via Sonogashira coupling of a substituted orthoaniline under aqueous conditions using Pd catalysis followed by acid-mediated cyclisation. The compounds were screened against the NCI-N87 and DLD-1 cancer cell lines, with most compounds showing low micromolar cytotoxic activity. |
| first_indexed | 2024-12-10T05:30:48Z |
| format | Article |
| id | doaj.art-554d381ba33343788b3eaf92e5787f3a |
| institution | Directory Open Access Journal |
| issn | 2405-8440 |
| language | English |
| last_indexed | 2024-12-10T05:30:48Z |
| publishDate | 2018-09-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Heliyon |
| spelling | doaj.art-554d381ba33343788b3eaf92e5787f3a2022-12-22T02:00:33ZengElsevierHeliyon2405-84402018-09-0149e00767Design, synthesis and evaluation of novel 2,2-dimethyl-2,3-dihydroquinolin-4(1H)-one based chalcones as cytotoxic agentsJulie Jean0David S. Farrell1Angela M. Farrelly2Sinead Toomey3James W. Barlow4Department of Chemistry, RCSI, 123 Stephen's Green, Dublin 2, IrelandDepartment of Chemistry, RCSI, 123 Stephen's Green, Dublin 2, IrelandDepartment of Medical Oncology, RCSI Education & Research Centre, Beaumont Hospital, Beaumont, Dublin 9, IrelandDepartment of Medical Oncology, RCSI Education & Research Centre, Beaumont Hospital, Beaumont, Dublin 9, IrelandDepartment of Chemistry, RCSI, 123 Stephen's Green, Dublin 2, Ireland; Corresponding author.We designed and synthesised a series of novel chalcones, incorporating the heterocyclic framework of 2,2-dimethyl-2,3-dihydro-4(1H)-quinolinone, which was prepared via Sonogashira coupling of a substituted orthoaniline under aqueous conditions using Pd catalysis followed by acid-mediated cyclisation. The compounds were screened against the NCI-N87 and DLD-1 cancer cell lines, with most compounds showing low micromolar cytotoxic activity.http://www.sciencedirect.com/science/article/pii/S2405844018327129Cancer researchPharmaceutical chemistry |
| spellingShingle | Julie Jean David S. Farrell Angela M. Farrelly Sinead Toomey James W. Barlow Design, synthesis and evaluation of novel 2,2-dimethyl-2,3-dihydroquinolin-4(1H)-one based chalcones as cytotoxic agents Heliyon Cancer research Pharmaceutical chemistry |
| title | Design, synthesis and evaluation of novel 2,2-dimethyl-2,3-dihydroquinolin-4(1H)-one based chalcones as cytotoxic agents |
| title_full | Design, synthesis and evaluation of novel 2,2-dimethyl-2,3-dihydroquinolin-4(1H)-one based chalcones as cytotoxic agents |
| title_fullStr | Design, synthesis and evaluation of novel 2,2-dimethyl-2,3-dihydroquinolin-4(1H)-one based chalcones as cytotoxic agents |
| title_full_unstemmed | Design, synthesis and evaluation of novel 2,2-dimethyl-2,3-dihydroquinolin-4(1H)-one based chalcones as cytotoxic agents |
| title_short | Design, synthesis and evaluation of novel 2,2-dimethyl-2,3-dihydroquinolin-4(1H)-one based chalcones as cytotoxic agents |
| title_sort | design synthesis and evaluation of novel 2 2 dimethyl 2 3 dihydroquinolin 4 1h one based chalcones as cytotoxic agents |
| topic | Cancer research Pharmaceutical chemistry |
| url | http://www.sciencedirect.com/science/article/pii/S2405844018327129 |
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