Design, synthesis and evaluation of novel 2, 2-dimethyl-2, 3-dihydroquinolin-4(1H)-one based chalcones as cytotoxic agents. Issue 9 (September 2018)

• Record Type: Journal Article
• Authors: Jean, Julie; Farrell, David S.; Farrelly, Angela M.; Toomey, Sinead; Barlow, James W.
• Is Part Of: Heliyon. Volume 4:Issue 9(2018)
• Publication Date: 2018-09
• Subjects: Cancer research -- Pharmaceutical chemistry; Research -- Periodicals; Medical sciences -- Periodicals; Natural history -- Periodicals; Social sciences -- Periodicals; Earth sciences -- Periodicals; Physical sciences -- Periodicals; 507.2
• DOI: 10.1016/j.heliyon.2018.e00767
• Languages: English
• ISSNs: 2405-8440

Abstract

Abstract: 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.