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ID: ALA1137238
Journal: Bioorg Med Chem Lett
Title: The synthesis and SAR of 2-amino-pyrrolo[2,3-d]pyrimidines: a new class of Aurora-A kinase inhibitors.
Authors: Moriarty KJ, Koblish HK, Garrabrant T, Maisuria J, Khalil E, Ali F, Petrounia IP, Crysler CS, Maroney AC, Johnson DL, Galemmo RA.
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 microM), anti-proliferative activity against several tumor cell lines and induces polyploidy in H460 cells.
CiteXplore: 16949284