To acquire a novel type of drug candidate with high anti-tumor potency for lung cancer, guided by the fragment-based drug design (FBDD), a string of new double MEK/PDK1 inhibitors was discovered through merging the functional structures of PD0325901 (a MEK inhibitor) and BX517 (a PDK1 inhibitor) (Fig. 1). Here, PDK1 is linked to lung carcinoma.