کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1362825 981497 2007 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
2,4,6-Trisubstituted pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure–activity relationship
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
2,4,6-Trisubstituted pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure–activity relationship
چکیده انگلیسی

Designed and synthesized were a series of pyridines substituted at 2, 4, and 6 positions with various 5- or 6-memberd heteroaromatics as antitumor agents. They were evaluated their topoisomerase I and II inhibitory activities along with cytotoxicities against several human cancer cell lines. Among the prepared compounds, 10–20 showed significant topoisomerase I or II inhibitory activities, and 21–26 showed considerable cytotoxicities against several human cancer cell lines. Structure–activity relationship study indicates that 4′-pyridine at 6-position of central pyridine plays a key role in biological activity.

Designed and synthesized were a series of pyridines substituted at 2, 4, and 6 positions with various 5- or 6-membered heteroaromatics as antitumor agents. They were evaluated for their topoisomerase I and II inhibitory activities along with cytotoxicities against several human cancer cell lines. Among the prepared compounds, 10–20 showed significant topoisomerase I or II inhibitory activity, and 21–26 showed considerable cytotoxicities against several human cancer cell lines. Structure–activity relationship study indicates that 4′-pyridine at 6-position of central pyridine plays a key role in biological activity.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 13, 1 July 2007, Pages 4351–4359
نویسندگان
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