The synthesis and characterization of new pyran derivatives (1–3) were realized by means of infrared spectroscopy (IR), 1H nuclearmagnetic resonance spectroscopy (1H NMR), high resolution mass spectrum (HRMS) and single crystal X-ray crystallography. The anti-proliferation activity of compounds 1–3 was investigated against human ovarian cancer cells CAOV3 by Cell Counting Kit-8 (CCK-8) assay. The RT-PCR assay was performed to detect the relative expression level of the Foxm1b in the CAOV3 cell line after treated with compounds 1–3. Furthermore, molecular docking studies supported the biological assay data and suggested that compared with compounds 1 and 3, compound 2 has stronger interaction with protein.