کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10900397 1084641 2005 12 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Structure-activity relationships of quassinoids for eukaryotic protein synthesis
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی تحقیقات سرطان
پیش نمایش صفحه اول مقاله
Structure-activity relationships of quassinoids for eukaryotic protein synthesis
چکیده انگلیسی
The effect of 63 quassinoids on eukaryotic protein synthesis has been investigated. Seventeen of the tested compounds showed potent in vitro activity, with IC50s below 2 μM for inhibition in Krebs ascites translation extracts. Sixteen of these quassinoids were also potent inhibitors of in vivo protein synthesis when exposed to Hela cells for 1 h. Our results led to the following structure-activity relationships for quassinoids regarding translation inhibition. Activity is influenced by (i) the nature of the C-15 side chain, (ii) the nature of A ring modifications, (iii) the presence or absence of a sugar moiety, and (iv) the presence of an epoxymethano bridge.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Cancer Letters - Volume 220, Issue 1, 18 March 2005, Pages 37-48
نویسندگان
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