Synthesis of apoptotic chalcone analogues in HepG2 human hepatocellular carcinoma cells

Cheon Soo Park; Yongchel Ahn; Dahae Lee; Sung Won Moon; Ki Hyun Kim; Noriko Yamabe; Gwi Seo Hwang; Hyuk Jai Jang; Heesu Lee; Ki Sung Kang; Jae Wook Lee

doi:10.1016/j.bmcl.2015.10.093

Synthesis of apoptotic chalcone analogues in HepG2 human hepatocellular carcinoma cells

Cheon Soo Park, Yongchel Ahn, Dahae Lee, Sung Won Moon, Ki Hyun Kim, Noriko Yamabe, Gwi Seo Hwang, Hyuk Jai Jang, Heesu Lee, Ki Sung Kang, Jae Wook Lee

Department of Pharmacy

Research output: Contribution to journal › Article › peer-review

11 Scopus citations

Abstract

Eight chalcone analogues were prepared and evaluated for their cytotoxic effects in human hepatoma HepG2 cells. Compound 5 had a potent cytotoxic effect. The percentage of apoptotic cells was significantly higher in compound 5-treated cells than in control cells. Exposure to compound 5 for 24 h induced cleavage of caspase-8 and -3, and poly (ADP-ribose) polymerase (PARP). Our findings suggest that compound 5 is the active chalcone analogue that contributes to cell death in HepG2 cells via the extrinsic apoptotic pathway.

Original language	English
Pages (from-to)	5705-5707
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	25
Issue number	24
DOIs	https://doi.org/10.1016/j.bmcl.2015.10.093
State	Published - 15 Dec 2015

Keywords

Anticancer
Apoptosis
Chalcone
HepG2

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10.1016/j.bmcl.2015.10.093

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title = "Synthesis of apoptotic chalcone analogues in HepG2 human hepatocellular carcinoma cells",

abstract = "Eight chalcone analogues were prepared and evaluated for their cytotoxic effects in human hepatoma HepG2 cells. Compound 5 had a potent cytotoxic effect. The percentage of apoptotic cells was significantly higher in compound 5-treated cells than in control cells. Exposure to compound 5 for 24 h induced cleavage of caspase-8 and -3, and poly (ADP-ribose) polymerase (PARP). Our findings suggest that compound 5 is the active chalcone analogue that contributes to cell death in HepG2 cells via the extrinsic apoptotic pathway.",

keywords = "Anticancer, Apoptosis, Chalcone, HepG2",

author = "Park, \{Cheon Soo\} and Yongchel Ahn and Dahae Lee and Moon, \{Sung Won\} and Kim, \{Ki Hyun\} and Noriko Yamabe and Hwang, \{Gwi Seo\} and Jang, \{Hyuk Jai\} and Heesu Lee and Kang, \{Ki Sung\} and Lee, \{Jae Wook\}",

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month = dec,

day = "15",

doi = "10.1016/j.bmcl.2015.10.093",

language = "English",

volume = "25",

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journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

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TY - JOUR

T1 - Synthesis of apoptotic chalcone analogues in HepG2 human hepatocellular carcinoma cells

AU - Park, Cheon Soo

AU - Ahn, Yongchel

AU - Lee, Dahae

AU - Moon, Sung Won

AU - Kim, Ki Hyun

AU - Yamabe, Noriko

AU - Hwang, Gwi Seo

AU - Jang, Hyuk Jai

AU - Lee, Heesu

AU - Kang, Ki Sung

AU - Lee, Jae Wook

PY - 2015/12/15

Y1 - 2015/12/15

N2 - Eight chalcone analogues were prepared and evaluated for their cytotoxic effects in human hepatoma HepG2 cells. Compound 5 had a potent cytotoxic effect. The percentage of apoptotic cells was significantly higher in compound 5-treated cells than in control cells. Exposure to compound 5 for 24 h induced cleavage of caspase-8 and -3, and poly (ADP-ribose) polymerase (PARP). Our findings suggest that compound 5 is the active chalcone analogue that contributes to cell death in HepG2 cells via the extrinsic apoptotic pathway.

AB - Eight chalcone analogues were prepared and evaluated for their cytotoxic effects in human hepatoma HepG2 cells. Compound 5 had a potent cytotoxic effect. The percentage of apoptotic cells was significantly higher in compound 5-treated cells than in control cells. Exposure to compound 5 for 24 h induced cleavage of caspase-8 and -3, and poly (ADP-ribose) polymerase (PARP). Our findings suggest that compound 5 is the active chalcone analogue that contributes to cell death in HepG2 cells via the extrinsic apoptotic pathway.

KW - Anticancer

KW - Apoptosis

KW - Chalcone

KW - HepG2

UR - https://www.scopus.com/pages/publications/84947280056

U2 - 10.1016/j.bmcl.2015.10.093

DO - 10.1016/j.bmcl.2015.10.093

M3 - Article

C2 - 26564263

AN - SCOPUS:84947280056

SN - 0960-894X

VL - 25

SP - 5705

EP - 5707

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 24

ER -

Synthesis of apoptotic chalcone analogues in HepG2 human hepatocellular carcinoma cells

Abstract

Keywords

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