title: Prodrugs of fluoro-substituted benzoates of EGC as tumor cellular proteasome inhibitors and apoptosis inducers.
abstract: The most potent catechin in green tea is (-)-epigallocatechin-3-gallate [(-)-EGCG], which, however, is unstable under physiological conditions. To discover more stable and more potent polyphenol proteasome inhibitors, we synthesized several novel fluoro-substituted (-)-EGCG analogs, named F-EGCG analogs, as well as their prodrug forms with all of -OH groups protected by acetate. We report that the prodrug form of one F-EGCG analog exhibited greater potency than the previously reported peracetate of (-)-EGCG to inhibit proteasomal activity, suppress cell proliferation, and induce apoptosis in human leukemia Jurkat T cells, demonstrating the potential of these compounds to be developed into novel anti-cancer and cancer-preventive agents.
authors.affiliation: The Prevention Program, Barbara Ann Karmanos Cancer Institute, and Department of Pathology, School of Medicine, Wayne State University, Detroit, Michigan, USA.|Shandong Tumor Hospital & Institute, Breast Cancer Center, Jinan, Shandong, China.
authors.forename: Zhiyong
authors.initials: Z
authors.lastname: Yu
authors.affiliation: Key Laboratory of Marine Drug, Ministry of Education, Medical College, Ocean University of China, Qingdao, China..
authors.forename: Xu Long
authors.initials: XL
authors.lastname: Qin
authors.affiliation: Key Laboratory of Marine Drug, Ministry of Education, Medical College, Ocean University of China, Qingdao, China..
authors.forename: Yan Yan
authors.initials: YY
authors.lastname: Gu
authors.affiliation: The Prevention Program, Barbara Ann Karmanos Cancer Institute, and Department of Pathology, School of Medicine, Wayne State University, Detroit, Michigan, USA.
authors.forename: Di
authors.initials: D
authors.lastname: Chen
authors.affiliation: The Prevention Program, Barbara Ann Karmanos Cancer Institute, and Department of Pathology, School of Medicine, Wayne State University, Detroit, Michigan, USA.
authors.forename: Qiuzhi Cindy
authors.initials: QC
authors.lastname: Cui
authors.affiliation: Key Laboratory of Marine Drug, Ministry of Education, Medical College, Ocean University of China, Qingdao, China..
authors.forename: Tao
authors.initials: T
authors.lastname: Jiang
authors.affiliation: Key Laboratory of Marine Drug, Ministry of Education, Medical College, Ocean University of China, Qingdao, China..
authors.forename: Sheng Biao
authors.initials: SB
authors.lastname: Wan
authors.affiliation: The Prevention Program, Barbara Ann Karmanos Cancer Institute, and Department of Pathology, School of Medicine, Wayne State University, Detroit, Michigan, USA.
authors.forename: Q Ping
authors.initials: QP
authors.lastname: Dou