5,6,-0-Isoalkylidene ascorbic acid derivatives

摘要

Novel condensation products between enediol ketolactones such as 5,6-0-isopropylidene ascorbic acid and 2-chloroethyl isocyanates are shown to have potent antitumor activity probably without the release of alkylating agents in vivo. While the structures of the products are not readily elucidated, activity is found to exceed that of BCNU (bis-(2-chloroethyl)-N-nitrosourea) and parallel that of the toxic and highly effective nitrosourea, MeCCNU (1-(4-trans-methylcyclohexyl)-3-(2-chloroethyl)-3-nitrosourea). Preferred compounds are condensation products of (A) wherein R2 and R3 are a lower alkyl group containing 1 to 3 carbon atoms or H and hal-CH2-CH2-N=C=O (B) wherein hal is I, Br or Cl.