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 ,
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
