Structure–activity study of epi-gallocatechin gallate (EGCG) analogs as proteasome inhibitors

[Display omitted] The structure–activity relationship of a number of synthetic green tea polyphenol analogs involving modifications of A ring and B ring of epi-gallocatechin gallate (EGCG) as proteasome inhibitors has been examined. It was found that in B ring, a decrease in the number of OH groups...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2005-03, Vol.13 (6), p.2177-2185
Main Authors: Wan, Sheng Biao, Landis-Piwowar, Kristin R., Kuhn, Deborah J., Chen, Di, Dou, Q. Ping, Chan, Tak Hang
Format: Article
Language:English
Subjects:
Biological and medical sciences
Catechin - analogs & derivatives
Catechin - chemical synthesis
Catechin - chemistry
Catechin - pharmacology
Flavonoids - chemical synthesis
Flavonoids - chemistry
Flavonoids - pharmacology
Inhibitory Concentration 50
Medical sciences
Miscellaneous
Molecular Structure
Pharmacology. Drug treatments
Phenols - chemical synthesis
Phenols - chemistry
Phenols - pharmacology
Polyphenols
Proteasome Endopeptidase Complex - metabolism
Proteasome Inhibitors
Stereoisomerism
Structure-Activity Relationship
Tea - chemistry
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Summary:[Display omitted] The structure–activity relationship of a number of synthetic green tea polyphenol analogs involving modifications of A ring and B ring of epi-gallocatechin gallate (EGCG) as proteasome inhibitors has been examined. It was found that in B ring, a decrease in the number of OH groups led to decreased potency. Introduction of a hydrophobic benzyl group into the 8 position of A ring did not significantly affect the proteasome-inhibitory potency.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2004.12.056