Anticancer activities of novel chalcone and bis-chalcone derivatives

被引:366
作者
Modzelewska, A
Pettit, C
Achanta, G
Davidson, NE
Huang, P
Khan, SR [1 ]
机构
[1] Johns Hopkins Univ, Sidney Kimmel Comprehens Canc Ctr, Div Chem Therapeut, Baltimore, MD 21231 USA
[2] Univ Texas, MD Anderson Canc Ctr, Dept Mol Pathol, Houston, TX 77030 USA
关键词
anticancer; chalcone; bis-chalcone; Claisen-Schmidt reaction;
D O I
10.1016/j.bmc.2006.01.003
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A series of novel chalcones and bis-chalcones containing boronic acid moieties has been synthesized and evaluated for antitumor activity against the human breast cancer MDA-MB-231 (estrogen receptor-negative) and MCF7 (estrogen receptor-positive) cell lines and against two normal breast epithelial cell lines, MCF-10A and MCF-12A. These molecules inhibited the growth of the human breast cancer cell lines at low micromolar to nanomolar concentrations, with five of them (1-4, 9) showing preferential inhibition of the human breast cancer cell lines. Furthermore, bis-chalcone 8 exhibited a more potent inhibition of colon cancer cells expressing wild-type p53 than of an isogenic cell line that was p53-null. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3491 / 3495
页数:5
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