Antitumor activity of novel fluoro-substituted (–)-epigallocatechin-3-gallate analogs
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چکیده
منابع مشابه
Structure-activity relationships of synthetic analogs of (-)-epigallocatechin-3-gallate as proteasome inhibitors.
BACKGROUND Cancer-related molecular targets of green tea polyphenols, such as (-)-epigallocatechin-3-gallate [(-)-EGCG], remain unknown. We previously showed that (-)-EGCG is a potent and specific inhibitor of the proteasomal chymotrypsin-like activity in vitro and in vivo. MATERIALS AND METHODS EGCG amides and five simple analogs were prepared by enantioselective synthesis. Proteasome inhibi...
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Background and Objective: The rate of survival in acute promyelocytic leukemia (APL) can dramatically improve, if the patients receive all-trans-retinoic acid (ATRA) treatment. However, this drugchr('39')s toxicity is a major problem in APL treatment. Previous researches have demonstrated that phyto-polyphenols such as epigallocatechin gallate (EGCG) and kaempferol cause apoptosis in hematopoie...
متن کاملMolecular Interactions between (−)-Epigallocatechin Gallate Analogs and Pancreatic Lipase
The molecular interactions between pancreatic lipase (PL) and four tea polyphenols (EGCG analogs), like (-)-epigallocatechin gallate (EGCG), (-)-gallocatechin gallate (GCG), (-)-epicatechin gallate (ECG), and (-)-epigallocatechin (EC), were studied from PL activity, conformation, kinetics and thermodynamics. It was observed that EGCG analogs inhibited PL activity, and their inhibitory rates dec...
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In view of potential biological activities of small molecule polyamides, we synthesized some novel N-(2-aminoethyl)-1-benzyl-2- (alkylthio)-1H-imidazole-5-carboxamide (7a,b), and N-(2-(1-benzyl-2-(alkylthio) -1H-imidazole- 5-carboxamido) ethyl)-1-benzyl-2- (alkylthio)-1H-imidazole-5-carboxamides (8a,b) as antitumor agents. The antitumor activity of compounds 7a,b and 8a,b was studied at c...
متن کاملAnticancer effects and molecular mechanisms of epigallocatechin-3-gallate
Epigallocatechin-3-gallate (EGCG) is a type of catechin found in green tea. EGCG exhibits a variety of activities, including anti-inflammatory, antidiabetes, antiobesity, and antitumor. In this review, we focus on the antitumor effects of EGCG. EGCG inhibits carcinogen activity, tumorigenesis, proliferation, and angiogenesis, and induces cell death. These effects are associated with modulation ...
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ژورنال
عنوان ژورنال: Cancer Letters
سال: 2010
ISSN: 0304-3835
DOI: 10.1016/j.canlet.2009.11.006