In conclusion, based on the importance of SIRT1 as a vital therapeutic target and the fact that the applications of “SIRT1-modulating autophagy” therapeutic strategy in brain cancer remains in its infancy, we innovatively discovered a novel small-molecule activator of SIRT1 with autophagic/mitophagic mechanisms, which has remarkable anti-tumor activity against glioblastoma in vitro and in vivo. The gene discussed is SIRT1; the disease is brain cancer.