Proteasome inhibition in human breast cancer cells with high catechol- O-methyltransferase activity by green tea polyphenol EGCG analogs

A pro-drug 8 of a synthetic analog 7 is more active in its antiproliferative activity against human breast cancer MDA-MB-231 cells possessing high catechol- O-methyltransferase (COMT) activity than the pro-drugs of EGCG and the analog 5. The higher activity of 8 is attributed to it not being a subst...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2010-02, Vol.18 (3), p.1252-1258
Main Authors: Huo, Congde, Yang, Huanjie, Cui, Qiuzhi Cindy, Dou, Q. Ping, Chan, Tak Hang
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents, Phytogenic - chemical synthesis
Antineoplastic Agents, Phytogenic - chemistry
Antineoplastic Agents, Phytogenic - pharmacology
Biological and medical sciences
Breast Neoplasms - drug therapy
Breast Neoplasms - enzymology
Catechin - analogs & derivatives
Catechin - chemical synthesis
Catechin - chemistry
Catechin - pharmacology
Catechol O-Methyltransferase - metabolism
Cell Survival - drug effects
Female
General aspects
General pharmacology
Humans
Medical sciences
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
Prodrugs - chemical synthesis
Prodrugs - chemistry
Prodrugs - pharmacology
Proteasome Endopeptidase Complex - metabolism
Proteasome Inhibitors
Tea - chemistry
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Summary:A pro-drug 8 of a synthetic analog 7 is more active in its antiproliferative activity against human breast cancer MDA-MB-231 cells possessing high catechol- O-methyltransferase (COMT) activity than the pro-drugs of EGCG and the analog 5. The higher activity of 8 is attributed to it not being a substrate of COMT.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2009.12.034