Synthesis of apoptotic chalcone analogues in HepG2 human hepatocellular carcinoma cells. Issue 24 (15th December 2015)

• Record Type: Journal Article
• Authors: Park, Cheon-Soo; Ahn, Yongchel; Lee, Dahae; Moon, Sung Won; Kim, Ki Hyun; Yamabe, Noriko; Hwang, Gwi Seo; Jang, Hyuk Jai; Lee, Heesu; Kang, Ki Sung; Lee, Jae Wook
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 24(2015)
• Page Start: 5705
• Page End: 5707
• Publication Date: 2015-12-15
• Subjects: Chalcone -- Anticancer -- HepG2 -- Apoptosis; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.10.093
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Eight chalcone analogues were prepared and evaluated for their cytotoxic effects in human hepatoma HepG2 cells. Compound5 had a potent cytotoxic effect. The percentage of apoptotic cells was significantly higher in compound5 -treated cells than in control cells. Exposure to compound5 for 24 h induced cleavage of caspase-8 and -3, and poly (ADP-ribose) polymerase (PARP). Our findings suggest that compound5 is the active chalcone analogue that contributes to cell death in HepG2 cells via the extrinsic apoptotic pathway.