کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1373938 981909 2009 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and bioactivity of a side chain bridged paclitaxel: A test of the T-Taxol conformation
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and bioactivity of a side chain bridged paclitaxel: A test of the T-Taxol conformation
چکیده انگلیسی

A knowledge of the bioactive tubulin-binding conformation of paclitaxel (Taxol™) is crucial to a full understanding of the bioactivity of this important anticancer drug, and potentially also to the design of simplified analogs. The bioactive conformation has been shown to be best approximated by the T-Taxol conformation. As a further test of this conclusion, the paclitaxel analog 4 was designed as a compound which has all the chemical functionality necessary for activity, but which cannot adopt the T-Taxol conformation. The synthesis and bioassay of 4 confirmed its lack of activity, and thus provided further support for the T-Taxol conformation as the bioactive tubulin-binding conformation.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 10, 15 May 2009, Pages 2884–2887
نویسندگان
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