Ursodeoxycholic acid (UDCA) and its derivatives were examined for anti-angiogenic activities by using the chick embryo chorioallantoic membrane (CAM) assay. The presence of UDCA or its derivatives inhibited angiogenesis in a dose-dependent manner; the dose required for half-maximal inhibition (ID50) was 4 microg per CAM for UDCA. The conjugate forms of UDCA with glycine methyl ester (HS-1030), L-leucine benzyl ester (HS-1068) and L-leucine methyl ester (HS-1133) were showing ID50 of 0.09, 0.08 and 0.6 microg per CAM, respectively. Also, the effect of UDCA and its derivatives on the viability of calf pulmonary artery endothelial (CPAE) cells was examined. Among them, HS-1030 effectively reduced the viability of CPAE cells in a concentration-dependent manner. Based on these results, we speculated that HS-1030 might be a promising candidate as angiogenesis inhibitor for use in the management of diseases accompanied by uncontrolled angiogenesis including solid tumor.