The Cytostatic Activity of the Chlorohyssopifolins, Chlorinated Sesquiterpene Lactones from Centaurea1

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Abstract
Five new chlorinated sesquiterpene lactones obtained from two species. of Compositae (Centaurea hyssopifolia Vahl and Centaurea linifolia Vahl) and another four closely-related lactone compounds were tested for cytostatic activity which was exhibited by four of the five new compounds. Studies of the chemical structure-activity relationship confirm the significance of an α-methylene-γ-lactone in these substances with regard to cytostatic activity which is further intensified by the presence of a chlorinated atom in the molecule. Chlorohyssopifolin C, the most potent of the series under study, appeared to operate chiefly upon the synthesis of DNA, the cytostatic activity of this lactone being found to be of an irreversible nature.

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