Synthesis of 3′-methoxy-E-diethylstilbestrol and its analogs as tumor angiogenesis inhibitors

► 3′-Methoxy-E-diethylstilbestrol (2) is a metabolite of diethylstilbestrol. ► 2 and its analogues (8 and 11) were synthesized as tumor angiogenesis inhibitors. ► The configuration was determined via the X-ray crystal diffraction of its derivative. ► 2, 8 and 11 showed potential anti-proliferation activities at a close level. ► The exposed hydroxyl-groups in the structures are required for their bioactivities.