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

Cited 88 time in scopus
Metadata Downloads
Title
Cytotoxic 2',5'-dihydroxychalcones with unexpected antiangiogenic activity
Author(s)
N H Nam; Y Kim; Y J You; Dong Ho Hong; Hwan Mook Kim; B Z Ahn
Bibliographic Citation
European Journal of Medicinal Chemistry, vol. 38, no. 2, pp. 179-187
Publication Year
2003
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% ?
Keyword
2′,5′-DihydroxychalconeAntiangiogenic activityAntitumor activityCytotoxicity
ISSN
0223-5234
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/S0223-5234(02)01443-5
Type
Article
Appears in Collections:
1. Journal Articles > Journal Articles
Files in This Item:
  • There are no files associated with this item.


Items in OpenAccess@KRIBB are protected by copyright, with all rights reserved, unless otherwise indicated.