Title of article
The synthesis and SAR of 2-amino-pyrrolo[2,3-d]pyrimidines: A new class of Aurora-A kinase inhibitors
Author/Authors
Kevin J. Moriarty، نويسنده , , Holly K. Koblish، نويسنده , , Thomas Garrabrant، نويسنده , , Jahanvi Maisuria، نويسنده , , Ehab Khalil، نويسنده , , Farah Ali، نويسنده , , Ioanna P. Petrounia، نويسنده , , Carl S. Crysler، نويسنده , , Anna C. Maroney، نويسنده , , Dana L. Johnson، نويسنده , , Robert A. Galemmo Jr.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
6
From page
5778
To page
5783
Abstract
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.
Keywords
Aurora-A , anti-proliferative , polyploidy , 3-d]pyrimidine
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797472
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