کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1365011 | 981550 | 2008 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
3-(Benzimidazol-2-yl)-pyridine-2-one-based ATP competitive inhibitors of Insulin-like Growth Factor 1 Kinase (IGF-IR) were optimized for reduced Cyp3A4 inhibition and improved oral exposure. The use of malonate as methyl anion synthon via SNAr reaction and double decarboxylation under mild conditions is demonstrated.
3-(Benzimidazol-2-yl)-pyridine-2-one-based ATP competitive inhibitors of Insulin-like Growth Factor 1 Kinase (IGF-IR) were optimized for reduced Cyp3A4 inhibition and improved oral exposure. The use of malonate as methyl anion synthon via SNAr reaction and double decarboxylation under mild conditions is demonstrated.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 14, 15 July 2008, Pages 4075–4080
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 14, 15 July 2008, Pages 4075–4080
نویسندگان
Kurt Zimmermann, Mark D. Wittman, Mark G. Saulnier, Upender Velaparthi, David R. Langley, Xiaopeng Sang, David Frennesson, Joan Carboni, Aixin Li, Ann Greer, Marco Gottardis, Ricardo M. Attar, Zheng Yang, Praveen Balimane, Lorell N. Discenza,