title: Structure-activity study of epi-gallocatechin gallate (EGCG) analogs as proteasome inhibitors.
abstract: 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.
authors.affiliation: Department of Applied Biology and Chemical Technology and the Open Laboratory of Chirotechnology, Institute of Molecular Technology for Drug Discovery and Synthesis, The Hong Kong Polytechnic University, Hung Hom, Hong Kong, SAR, China.
authors.forename: Sheng Biao
authors.initials: SB
authors.lastname: Wan
authors.forename: Kristin R
authors.initials: KR
authors.lastname: Landis-Piwowar
authors.forename: Deborah J
authors.initials: DJ
authors.lastname: Kuhn
authors.forename: Di
authors.initials: D
authors.lastname: Chen
authors.forename: Q Ping
authors.initials: QP
authors.lastname: Dou
authors.forename: Tak Hang
authors.initials: TH
authors.lastname: Chan
mesh_terms: D002392:Catechin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D005419:Flavonoids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010636:Phenols / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D059808:Polyphenols; D046988:Proteasome Endopeptidase Complex / Q000378:metabolism; D061988:Proteasome Inhibitors; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013662:Tea / Q000737:chemistry*
chemical_list: D005419:Flavonoids; D010636:Phenols; D059808:Polyphenols; D061988:Proteasome Inhibitors; D013662:Tea; C417940:gallocatechin gallate; D002392:Catechin; D046988:Proteasome Endopeptidase Complex