Design, stereoselective synthesis, and antitumoral activity of combretastatin A-4 analogs

Combretastatin A-4 (CA-4) is a microtubule targeting agent, and it has a great advantage when compared to other compounds with a similar mechanism of action, such as vinca alkaloids, colchicine, podophillotoxin, and paclitaxel: its simpler structure. In this work, the stereoselective synthesis and antiproliferative activity of stable CA-4 analogs, obtained from the cross-coupling reaction between vinyl tellurides and potassium aryltrifluoroborates is described. The method is simple, fast, and general, allowing further applications for the synthesis of more complex compounds.