کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1356949 | 981177 | 2007 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Optimization and determination of the absolute configuration of a series of potent inhibitors of human papillomavirus type-11 E1–E2 protein–protein interaction: A combined medicinal chemistry, NMR and computational chemistry approach
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
We have previously reported the discovery and initial SAR optimization of the first series of inhibitors of the human papillomavirus type-11 (HPV11) E1–E2 protein–protein interaction. These inhibitors featured an indandione system spiro-fused onto an all syn substituted tetrahydrofuran ring. In this paper, we report new SAR efforts which have led to the identification of the first low nanomolar inhibitor of the HPV11 E1–E2 protein–protein interaction. In addition, we report a combined NMR and computational chemistry approach which allowed the successful determination of the absolute stereochemistry of the active species originating from the initial racemic lead.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 7, 1 April 2007, Pages 2690–2700
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 7, 1 April 2007, Pages 2690–2700
نویسندگان
Nathalie Goudreau, Dale R. Cameron, Robert Déziel, Bruno Haché, Araz Jakalian, Eric Malenfant, Julie Naud, William W. Ogilvie, Jeff O’Meara, Peter W. White, Christiane Yoakim,