Compounds 3a and 3b (Figure 2) blocked FAK in enzymatic assay with comparable activity to TAE226 (IC50 = 5.17 nM and = 2.58 nM, respectively), showed potent anticancer activity against different cancer cells (AsPC-1 cells, BxPC-3 cells, and MCF-7/ADR cells) and displayed antiproliferative action in an in vivo xenograft mouse model. Here, PTK2 is linked to cancer.