Abstract:

Combretastatin A-4 (CA-4) (Figure 1), a natural Zstilbene isolated from the South African willow Combretum caffrum, has been found to strongly inhibit the tubulin assembly by binding to the colchicine site and to be a cytotoxic agent against a wide variety of cell lines, including multidrugresistant lines. The structural simplicity of CA-4 combined with its excellent antitumor and antivascular activities encouraged the scientific community to synthesize numerous analogs. From these structure–activity relationship (SAR) investigations, it has been established that the cis-orientation of the two aryl rings is crucial for the activity of CA-4 as well as the trimethoxyaryl unit, whereas, the hydroxyl group on the 3’-position is not essential. Consequently, the synthesis of CA-4 analogs for further studies of their biological activities is of the great interest.