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...

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Bibliographic Details
Published inHeliyon Vol. 4; no. 9; p. e00767
Main Authors Jean, Julie, Farrell, David S., Farrelly, Angela M., Toomey, Sinead, Barlow, James W.
Format Journal Article
LanguageEnglish
Published England Elsevier Ltd 01.09.2018
Elsevier
Subjects
Cancer research
Pharmaceutical chemistry
Pharmaceutical chemistry
Cancer research
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Summary: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.
Bibliography:ObjectType-Article-1
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ISSN:2405-8440
2405-8440
DOI:10.1016/j.heliyon.2018.e00767