کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1392448 | 1501133 | 2014 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and antiproliferative activity of novobiocin analogues as potential hsp90 inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
• A new series of novobiocin analogues was designed and synthesized.
• Compound 2b showed GI50 values at a micromolar level in various human cancer cells.
• 2b is a potent inducer of G2/M arrest as well as apoptosis.
• 2b is able to induce proteasome-mediated degradation of ERα.
A series of substituted coumarins1–10 was designed and synthesized as a novel class of 4TCNA analogues. Compound 2a showed excellent antiproliferative activity with mean GI50 values at a micromolar level in a diverse set of human cancer cells (GI50 = 2–30 μM) and induced a high apoptosis level in MCF-7 breast cancer cell line. The molecular signature of hsp90 inhibition was assessed by depletion of the Erα hsp90 client protein.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 83, 18 August 2014, Pages 498–507
Journal: European Journal of Medicinal Chemistry - Volume 83, 18 August 2014, Pages 498–507
نویسندگان
Davide Audisio, Délphine Methy-Gonnot, Christine Radanyi, Jack-Michel Renoir, Stéphanie Denis, Félix Sauvage, Juliette Vergnaud-Gauduchon, Jean-Daniel Brion, Samir Messaoudi, Mouad Alami,