Abstract: An novel bisbibenzyl derivative was totally synthesized from 3, 4-dimethoxy-6-bromobenzaldehyde, 3-hydroxy-4-methoxybenzaldehyde, 2-hydroxy-3-methoxybenzaldehyde and 4-bromobenzoic acid methyl ester, throuth Ullmann reaction, aldehyde group reduction, phosphorus salt formation, Wittig reaction, intramolecular Wittig reaction, phenolic hydroxy and aldehyde group protection and deprotection as well as catalytic hydrogenation of alkene reaction. The structures of the compounds were confirmed by MS and ¹H NMR. The effects of the target compounds on the proliferation of U2OS cells and YFP cells were evaluated in vitro by MTT assay using marchantin C as the positive control, and the results showed stronger activity of the target product than that of the marchantin C.