کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1367310 | 981625 | 2006 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The synthesis and SAR of 2-amino-pyrrolo[2,3-d]pyrimidines: A new class of Aurora-A kinase inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A new class of Aurora-A inhibitors have been identified based on the 2-amino-pyrrolo[2,3-d]pyrimidine scaffold. Here, we describe the synthesis and SAR of this novel series. We report compounds which exhibit nanomolar activity in the Aurora-A biochemical assay and are able to inhibit tumor cell proliferation. This study culminates in compound 30, an inhibitor with potent activity against Aurora A (IC50 = 0.008 μM), anti-proliferative activity against several tumor cell lines and induces polyploidy in H460 cells.
The synthesis of a potent Aurora-A inhibitor 32 (IC50 = 0.8 nm) is reported.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 22, 15 November 2006, Pages 5778–5783
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 22, 15 November 2006, Pages 5778–5783
نویسندگان
Kevin J. Moriarty, Holly K. Koblish, Thomas Garrabrant, Jahanvi Maisuria, Ehab Khalil, Farah Ali, Ioanna P. Petrounia, Carl S. Crysler, Anna C. Maroney, Dana L. Johnson, Robert A. Galemmo Jr.,