کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1361847 981472 2007 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, syntheses, and antitumor activity of novel chromone and aurone derivatives
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design, syntheses, and antitumor activity of novel chromone and aurone derivatives
چکیده انگلیسی

A series of new chromone analogues bearing heterocyclic thioether moiety and aurone analogues bearing cyclic tertiary amine moiety were designed and synthesized under microwave irradiation. The synthetic protocol was found to present many advantages, such as higher yields, shorter reaction time (10–20 min), mild condition, and readily isolation of the products. The synthesized compounds were assayed for their antitumor activity against four kinds of human solid tumor cell lines including HCCLM-7, Hep-2, MDA-MB-435S, and SW-480. Two compounds, (Z)-2-((4-benzyl-piperazin-1-yl)methylene)benzofuran-3(2H)-one 5e and (Z)-2-((4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)methylene)benzofuran-3(2H)-one 5f, were identified as the most promising candidates with the IC50 values in the range of 4.1–13.1 μM. Further cell cycle studies revealed that compounds 5e and 5f arrest the cell cycle in G0/G1 phase and displayed apoptosis-inducing effect on Hep-2 cells.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 15, 1 August 2007, Pages 5191–5197
نویسندگان
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