کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1397233 1501114 2015 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Antitumor activity of endoperoxide-iron chelator conjugates―design, synthesis and biological evaluation
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Antitumor activity of endoperoxide-iron chelator conjugates―design, synthesis and biological evaluation
چکیده انگلیسی


• These endoperoxide and iron chelator conjugates inhibited cancer cell proliferation.
• These compounds displayed 2–4 fold selectivity against cancer cell vs normal cell.
• Both endoperoxide and iron-chelating moiety contributed to the biological ability.

The effort to pursue effective anti-cancer drugs with novel mechanism of action has been continued for decades. As an antimalarial agent, artemisinin is well-known for its endoperoxide moiety, which is activated by the cellular iron. Meanwhile, the anti-cancer activity of artemisinin is recognized and reported. Herein, we report on the design, synthesis and evaluation of a series of endoperoxide and iron chelating moiety conjugates. Our study demonstrated that the endoperoxide-quinoline conjugates displayed effective antiproliferative capability and good selectivity against certain cancer cells, while both hydroxamate and catechol-endoperoxide conjugates shown no significant inhibitory activity. Preliminary mechanism investigation suggested that the antiproliferative activity of these conjugates is related to the endoperoxide moiety as well as their iron-chelating ability. These compounds are expected to be used as prototype for further development of selective anti-cancer drug candidate.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 102, 18 September 2015, Pages 180–187
نویسندگان
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