Synthesis and evaluation of curcumin analogues as potential thioredoxin reductase inhibitors |
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Authors: | Qiu Xu Liu Zhong Shao Wei-Yan Liu Xing Jing Da-Ping Yu Yan-Jun An Lin-Kun Huang Shi-Liang Bu Xian-Zhang Huang Zhi-Shu Gu Lian-Quan |
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Institution: | School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510275, China. |
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Abstract: | 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. |
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