کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1362710 981494 2010 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis, metabolism and in vitro cytotoxicity studies on novel lavendamycin antitumor agents
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis, metabolism and in vitro cytotoxicity studies on novel lavendamycin antitumor agents
چکیده انگلیسی

A series of lavendamycin analogues with two, three or four substituents at the C-6, C-7 N, C-2′, C-3′ and C-11′ positions were synthesized via short and efficient methods and evaluated as potential NAD(P)H:quinone oxidoreductase (NQO1)-directed antitumor agents. The compounds were prepared through Pictet–Spengler condensation of the desired 2-formylquinoline-5,8-diones with the required tryptophans followed by further needed transformations. Metabolism and toxicity studies demonstrated that the best substrates for NQO1 were also the most selectively toxic to NQO1-rich tumor cells compared to NQO1-deficient tumor cells.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 18, Issue 5, 1 March 2010, Pages 1899–1909
نویسندگان
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