We have investigated the antiproliferative and cytotoxic effects of selected enediynes against three Kaposi's sarcoma (KS) cell lines. The enediynes tested were found to be very potent in inhibiting the growth of KS cells. Treatment with concentrations of 10(-10) M or less were capable of producing 50% inhibition of growth. Furthermore, treatment of KS cells with enediynes induced apoptosis in up to 80% of the cells. This unique class of antitumor agents has therapeutic potential for the treatment of KS.