The Annonaceous acetogenins are promising new antitumor and pesticidal agen
ts that are found only in the plant family Annonaceae. Chemically, they are
derivatives of long-chain fatty acids. Biologically, they exhibit their po
tent bioactivities through depletion of ATP levels via inhibiting complex I
of mitochondria and inhibiting the NADH oxidase of plasma membranes of tum
or cells. Thus, they thwart ATP-driven resistance mechanisms. This review p
resents the progress made in the chemistry, biology, and development of the
se compounds since December 1995.