Structure-activity study of epi-gallocatechin gallate (EGCG) analogs as proteasome inhibitors.
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.
Wan
Sheng Biao
SB
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.
Landis-Piwowar
Kristin R
KR
Kuhn
Deborah J
DJ
Chen
Di
D
Dou
Q Ping
QP
Chan
Tak Hang
TH
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*
D005419:Flavonoids; D010636:Phenols; D059808:Polyphenols; D061988:Proteasome Inhibitors; D013662:Tea; C417940:gallocatechin gallate; D002392:Catechin; D046988:Proteasome Endopeptidase Complex