Chartarolides A–C (25–27) exhibited remarkable cytotoxic activities against the HCT-116, HepG2, BGC-823, NCI-H1650, A2780, and MCF7 human tumor cell lines with IC50 values around 1.3 to 12.5 μM and showed strong inhibitory activities against the human tumor-related protein kinases of FGFR3, IGF1R, PDGFRb, and TrKB with IC50 values ranging from 2.6 to 20.3 μM. Here, IGF1R is linked to neoplasm.