5,6,-0-Isoalkylidene ascorbic acid derivatives

Details 5,6,-0-Isoalkylidene ascorbic acid derivatives 5,6,-0-Isoalkylidene ascorbic acid derivatives

1981-10-23

1983-12-27

Love, Ethel G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

549315, 549317, 549318, 549321, 424280, C07D40700, C07D30762

Patent

active

044232365

ABSTRACT:
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 ##STR1## wherein R.sub.2 and R.sub.3 are a lower alkyl group containing 1 to 3 carbon atoms or H and

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Johnston et al., Journ. Med. Chem., Jul. 1971, pp. 600-614.

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