The discovery and invention of new type of anti-angiogenesis agents are very important for the treatment of a variety of tumors due to a fact that growth and metastasis of tumor highly depended upon angiogenesis. Cortistatin A and its analogues are a new kind of steroidal alkaloids with 9-(10,19)-abeo-androstane skeleton and a bridged seven-membered B ring of marine origin. Cortistatin A shows cytostatic anti-proliferative activity against human umbilical vein endothelial cell (HUVEC) at very wide range concentrations (100 pmol/L to 1 μmol/L), in which the selective index is more than 3300-fold higher in comparison with those of several other cell lines. This review summarizes the synthetic progress of cortistatin A and its analogues since their discovery in 2006～2007.

Key words: steroidal alkaloid, anti-angiogensis, antitumor, synthesis, cortistatin