表没食子儿茶素没食子酸酯类似物通过抑制儿茶酚-O-甲基转移酶活性对人乳腺癌细胞蛋白酶体的抑制作用。
Proteasome inhibition in human breast cancer cells with high catechol-O-methyltransferase activity by green tea polyphenol EGCG analogs.
机构信息
Department of Chemistry, McGill University, Montreal, Quebec, Canada.
出版信息
Bioorg Med Chem. 2010 Feb;18(3):1252-8. doi: 10.1016/j.bmc.2009.12.034. Epub 2009 Dec 16.
Abstract
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.
摘要
一种合成类似物 7 的前药 8 在抗具有高儿茶酚-O-甲基转移酶（COMT）活性的人乳腺癌 MDA-MB-231 细胞的增殖活性方面比 EGCG 的前药和类似物 5 更有效。8 的更高活性归因于它不是 COMT 的底物。
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