کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1373428 1500544 2010 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
N-Aryl-benzimidazolones as novel small molecule HSP90 inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
N-Aryl-benzimidazolones as novel small molecule HSP90 inhibitors
چکیده انگلیسی

We describe the development of a novel series of N-aryl-benzimidazolone HSP90 inhibitors (9) targeting the N-terminal ATP-ase site. SAR development was influenced by structure-based design based around X-ray structures of ligand bound HSP90 complexes. Lead compounds exhibited high binding affinities, ATP-ase inhibition and cellular client protein degradation.

We describe the development of a novel series of N-aryl-benzimidazolone HSP90 inhibitors targeting the N-terminal ATP-ase site. SAR development was influenced by structure-based design based around X-ray structures of ligand bound HSP90 complexes. Lead compounds exhibited high binding affinities, ATP-ase inhibition and cellular client protein degradation.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 24, 15 December 2010, Pages 7503–7506
نویسندگان
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