کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1364509 981538 2007 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
The concise synthesis of chalcone, indanone and indenone analogues of combretastatin A4
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
The concise synthesis of chalcone, indanone and indenone analogues of combretastatin A4
چکیده انگلیسی

A series of aryl- and aroyl-substituted chalcone analogues of the tubulin binding agent combretastatin A4 (1) were prepared, using a recently introduced one-pot palladium-mediated hydrostannylation-coupling reaction sequence. These chalcones were converted to indanones by Nazarov cyclisation, followed by oxidation to give the corresponding indenones. Indenones were also prepared using a palladium-mediated formal [3+2]-cycloaddition process between ortho-halobenzaldehydes and diarylpropynones. All compounds were assessed as inhibitors of tubulin polymerisation, but only E-31 had activity similar to that of 1. However, compound E-31 did not exhibit antiproliferative activity against the MCF-7 cell line.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 9, 1 May 2007, Pages 3290–3298
نویسندگان
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