SYNTHESIS OF SOME IDEOXY-ALPHA,BETA-L-GLYCERO-TETRURONO-1,4-LACTONES - EVALUATION AS ANTITUMOR AGENTS

A series of -dideoxy-5-O-trityl-D-erythro-pentono-1,4-lactones were de tritylated. The resultant free-hydroxy compounds Were converted to the ir respective ideoxy-alpha,beta-L-glycero-tetrurono-1,4-lactones (L-su gar numbering) in a one-vessel reaction sequence of (a) conversion of the lactones to their aldonic acid sodium salts, (b) cleavage of the r esulting aldonates with sodium metaperiodate, and (c) acidification, f ollowed by acetylation, to give the title compounds. The unsubstituted tetrurono-1,4-lactones were inhibitory toward L1210 leukemia cells at concentrations in the 10(-4) M range.