Abstract: AIM: To synthesize some new analogues of α-DDB (dimethyl 4,4′-dimethoxy-5,6,5′,6′-dimethylenedioxy-2,2′-biphenyl dicarboxylate). METHODS: Structure modification to the carbomethoxy of α-DDB to synthesize some symmetrical and asymmetrical biphenyl anlogues. The structures of these compounds are confirmed by IR, ¹HNMR, MS and EA. RESULTS: Nine dirivatives of α-DDB have been synthesized and three of them (3, 4 and 5) are new compounds. CONCLUSION: Most of these compounds have antitumor activities.