کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1363445 981512 2007 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Acridone derivatives: Design, synthesis, and inhibition of breast cancer resistance protein ABCG2
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Acridone derivatives: Design, synthesis, and inhibition of breast cancer resistance protein ABCG2
چکیده انگلیسی

The breast cancer resistance protein (BCRP, ABCG2) is among the latest discovered ABC proteins to be involved in MDR phenotype and for which only few inhibitors are known. In continuing our program aimed at discovering efficient multidrug resistance modulators, we conceived and synthesized new acridones as ABCG2 inhibitors. The design of target molecules was based on earlier results dealing with ABCG2 inhibition with flavone and chromone derivatives. The human wild-type (R482) ABCG2-transfected cells were used for rational screening of inhibitory acridones. The synthesis of target compounds, the inhibitory activity against ABCG2, and structure–activity relationships are described. One of the acridones was even more potent than the reference inhibitor, GF120918, as shown by its ability to inhibit mitoxantrone efflux.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 8, 15 April 2007, Pages 2892–2897
نویسندگان
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