期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 16, 期 17, 页码 8035-8041出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.07.054
关键词
curcumin derivatives; TrxR inhibitor; furan moiety
资金
- The Education Ministry of PR China [105133]
- Guangdong Provincial Natural Science Foundation [5001773]
- The Hong Kong Polytechnic University Area of Strategic Development Fund
Series of curcumin derivatives were synthesized; the inhibitory activities on thioredoxin reductase (TrxR) of all analogues were evaluated by DTNB assay in vitro. It is found that most of the analogues can inhibit TrxR in the low micromolar range; Structure-activity relationship analysis reveals that analogues with furan moiety have excellent inhibitory effect on TrxR in an irreversible manner, indicating that the furan moiety may serve as a possible pharmacophore during the interaction of curcumin analogues with TrxR. The effect of selected curcuminoids on growth of different TrxR overexpressed cancer cell lines was also investigated and discussed. (C) 2008 Elsevier Ltd. All rights reserved.
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