Mitochondria targeting combined with methyl modification of novel resveratrol derivatives enhances anti-tumor activity†

Mitochondria-targeting methyl modification compounds A1–A6 were synthesized by introducing TPP⁺ into the pharmacophore. A4 ((E)-Triphenyl(4-(4-(3,4-dimethylstyryl)phenoxy)butyl)phosphoniumiodide) could selectively accumulate in the mitochondria and exert excellent anticancer activity by both cell cycle arrest in G0/G1 and apoptosis induction in the mitochondrial pathway. The target mitochondria drug design is an effective strategy for exploiting the drug potential for cancer therapy.