کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1356413 981116 2010 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis and biological evaluation of chrysin long-chain derivatives as potential anticancer agents
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design, synthesis and biological evaluation of chrysin long-chain derivatives as potential anticancer agents
چکیده انگلیسی

A series of long-chain derivatives of chrysin (compounds 3–22) were synthesized to evaluate for their antiproliferative activities against the human liver cancer cell line HT-29 and EGFR inhibitory activity. Among the compounds tested, compounds hexadecyl 2-(5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yloxy)acetate (10) and N-hexadecyl 2-(5-hydroxy-4-oxo-2-phenyl-4H-chromen-7-yloxy)acetamide (20) displayed potent EGFR inhibitory activity with IC50 values of 0.048 μM and 0.035 μM), comparable to the positive control erlotinib. Docking simulation of compounds 10 and 20 was carried out to illustrate the binding mode of the molecular into the EGFR active site, and the result suggested that compound 10 and 20 can bind the EGFR kinase well. Thus, compounds 10 and 20 with potent EGFR inhibitory activity would be potential anticancer agents.

A series of long-chain derivatives of chrysin (compounds 3–22) were synthesized to evaluate for their antiproliferative activities against the human liver cancer cell line HT-29 and EGFR inhibitory activity. Compounds 10 and 20 displayed potent EGFR inhibitory activity with IC50 values of 0.048 μM and 0.035 μM, comparable to the positive control erlotinib.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 18, Issue 3, 1 February 2010, Pages 1117–1123
نویسندگان
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