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
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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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
Journal: Bioorganic & Medicinal Chemistry - Volume 18, Issue 5, 1 March 2010, Pages 1899–1909
نویسندگان
Wen Cai, Mary Hassani, Rajesh Karki, Ervin D. Walter, Katherine H. Koelsch, Hassan Seradj, Jayana P. Lineswala, Hamid Mirzaei, Jeremy S. York, Fatemeh Olang, Minoo Sedighi, Jennifer S. Lucas, Thomas J. Eads, Anthony S. Rose, Sahba Charkhzarrin,