Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1367310 | Bioorganic & Medicinal Chemistry Letters | 2006 | 6 Pages |
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.
Graphical abstractThe synthesis of a potent Aurora-A inhibitor 32 (IC50 = 0.8 nm) is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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.,