کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1372197 981867 2009 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Cancer preventive agents 9. Betulinic acid derivatives as potent cancer chemopreventive agents
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Cancer preventive agents 9. Betulinic acid derivatives as potent cancer chemopreventive agents
چکیده انگلیسی

C-3 esterifications of betulinic acid (BA, 1) and its A-ring homolog, ceanothic acid (CA, 2), were carried out to provide sixteen terpenoids, 4–19, including nine new compounds (4–12). All synthesized compounds were evaluated in an in vitro antitumor-promoting assay using the Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells. Among them, compounds 4–6, 11–14, 16, and 17 displayed remarkable inhibitory effects of EBV-EA activation. BA analog 6, which contains a prenyl-like group, showed the most potent inhibitory effect (100%, 76%, 37%, and 11% inhibition of EBA activation at 1000, 500, 100, and 10 mol ratio/TPA, respectively, with IC50 value of 285 mol ratio/32 pmol TPA). Compound 6 merits further development as a cancer preventive agent.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 13, 1 July 2009, Pages 3378–3381
نویسندگان
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