Abstract: 3-(4-Hydroxyphenyl)-4-methyl-6-methoxy-7-hydroxycoumarin (2a) and its analogues with different substituents at the p-position of 3-phenyl group were designed and synthesized as the non-steroidal analogues of 2-methoxyestradiol (2-ME 1). The desired compounds were synthesized via a novel and simple route and the effects of specific substituents on their anti-angiogenesis activities were investigated with Human umbilical vein endothelial cells (HUVECs) proliferation assays. Preliminary biological screening showed that compounds 2a and 2d (IC50 = 61.0 and 76.7 μM, respectively) have potential anti-angiogenesis activities. The bulk of the group at the p-position of 3-phenyl group likely play an important role in their activities.

Key words: Angiogenesis inhibitor, 2-Methoxyestradiol, Non-steroidal analogue, 3-(4-Hydroxyphenyl)-4-methyl-6-methoxyl-7-hydroxycoumarin