A series of 2-amino-9-aryl-7H-pyrrolo [2, 3-d] pyrimidines were designed and synthesized to target focal adhesion kinase (FAK). A number of these pyrrolopyrimides exhibited low micromolar inhibitory activities against focal adhesion kinase, and their preliminary SAR was established via systematic chemical modifications. The 2-amino-9-aryl-7H-pyrrolo [2, 3-d] pyrimidines represent a new class of kinase inhibitors.