期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 17, 期 3, 页码 1109-1117出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.12.044
关键词
Estrogen receptor; Agonists; Carborane; Phenols; Structure-activity relationship
资金
- High Technology Research Program [16390032]
- Ministry of Education, Culture, Sports, Science and Technology, Japan [18790089]
- Grants-in-Aid for Scientific Research [18790089, 20390035, 21790116] Funding Source: KAKEN
p-Carborane bisphenols and their derivatives were prepared and evaluated for binding affinity to estrogen receptor alpha. Their estrogenic activity was evaluated by means of transcriptional assay and cell proliferation assay using MCF-7 cell lines. 1,12-Bis(4-hydroxyphenyl)-1,12-dicarba-closo-dodecaborane 4a showed potent estrogenic activity, approaching that of 17 beta-estradiol, in transactivation assay. The activity of isomers 5a and 6a was drastically affected by the change in the position of one of the hydroxyl groups; 6a (ortho-OH in one ring) was about 1000 times less potent than 4a. Modification of this hydroxyl group with alkyl groups decreased the estrogenic activity in all isomers. Compound 4a also showed potent MCF-7 cell proliferation-enhancing activity. (C) 2008 Elsevier Ltd. All rights reserved.
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