Chalcone Derivatives Inhibit Glutathione S-Transferase P1-1 Activity: Insights into the Interaction Mode of , β-Unsaturated Carbonyl Compounds

来自 EBSCO

阅读量:

71

作者:

J WangS WangD SongD ZhaoY ShaY JiangY JingM Cheng

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摘要:

Resistance to chemotherapeutic drugs has long been a considerable barrier to successful treatment of many cancers and over-expression of glutathione S-transferase P1-1 is correlated to carcinogenesis and resistance of cancer cells against chemotherapeutic agents. This study throws light on the role of chalcone derivatives, a new class of glutathione S-transferase P1-1 inhibitors potentially to overcome glutathione S-transferase P1-1-mediated chemotherapy resistance. Nineteen α-substituted chalcone derivatives were synthesized and their in vitro inhibitory effects on glutathione S-transferase P1-1 were determined. We interestingly found that most of these compounds showed inhibitory effect on glutathione S-transferase P1-1 activity. In addition, molecular field-based similarity analysis provides the necessary three-dimensional molecular field properties of α, β-unsaturated carbonyl derivatives to inhibit glutathione S-transferase P1-1 activity. Thus, these compounds hav

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DOI:

10.1111/j.1747-0285.2009.00807.x

被引量:

7

年份:

2009

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