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Title 

Cytotoxic 2',5'-dihydroxychalcones with unexpected antiangiogenic activity

Authors 

N H NamY KimY J YouDong Ho HongHwan Mook KimB Z Ahn

Publisher 

Elsevier

Issue Date 

2003

Citation 

European Journal of Medicinal Chemistry, vol. 38, no. 2, pp. 179-187

Keywords 

2′,5′-dihydroxychalconeantiangiogenic activityantitumor activitycytotoxicityantineoplastic activitydrug activitystructure activity relationstructure-activity relationship

Abstract 

A series of 2′,5′-dihydroxychalcones were synthesized and evaluated for cytotoxicity against tumor cell lines and human umbilical venous endothelial cells (HUVEC). It was found that chalcones with electron-withdrawing substituents on the B ring exhibited potent cytotoxicity against a variety of tumor cell lines while compounds with electron-releasing groups were less potent in general. Those compounds with B ring replaced by extended or heteroaromatic rings exhibited significant bioactivity. Several compounds were shown to have marked cytotoxic selectivity towards HUVECs. Especially, among the synthesized compounds, 2-chloro-2′,5′-dihydroxychalcone (2-3) showed the highest selectivity index up to 66 in comparison to HCT116 cells. This compound also exhibited strong inhibitory effects on the HUVEC tube formation in an in vitro model. When administered into BDF1 mice bearing Lewis lung carcinoma cells at 50 mg kg-1 day-1, 2-3 was found to inhibit the growth of tumor mass by 60.5%

ISSN 

0223-5234

Link 

http://dx.doi.org/10.1016/S0223-5234(02)01443-5

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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