It can be isolated from Combretum afrum, the Eastern Cape South African bushwillow tree or in Combretum leprosum, the mofumbo, a species found in Brazil.

[2][3] Tubulin represents a potent target in cancer chemotherapy, given its role in cell division.

Combretastatin is a naturally occurring well known tubulin polymerization inhibitor.

[4] Combretastatin A-4 is the active component of combretastatin A-4 phosphate, a prodrug designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis.

[citation needed] A large number of synthetic derivatives have been reported,[5][6] including beta-lactam based compounds.