Given the severity of most cancers and their high unmet clinical need, together with the fact that the PI3K-Akt-mTOR axis represents an important emerging class of drug targets, we designed and synthesized a series of hybrids of α-methylene-γ-lactones and 2-phenyl indoles with the aim of discovery of new inhibitor(s) targeting PI3K-Akt-mTOR pathway [8]. The gene discussed is MTOR; the disease is cancer.