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Naturally occurring cytotoxic compounds have been considered to be a valuable pool of lead compounds in the development of potential anticancer drugs. Currently, some cytotoxic compounds of terrestrial plants are being used as cancer therapeutic drugs and more candidates are under clinical trials along with cytotoxic small molecules of terrestrial microorganisms and marine organisms. In the present review, the structures and representative cytotoxicities of new organic small molecules (over 200 molecules) obtained from terrestrial plants between 2001 and 2004 are presented.