K. Shyam et al., THIOLYSABLE PRODRUGS OF 1,2-BIS(METHYLSULFONYL)-1-(2-CHLOROETHYL)HYDRAZINE WITH ANTINEOPLASTIC ACTIVITY, European journal of medicinal chemistry, 33(7-8), 1998, pp. 609-615
Several 2-alkoxycarbonyl- and 2-aryloxycarbonyl-1,2-bis(methylsulfony1
)-1- (2-chloroethyl)hydrazines, conceived as thiolysable prodrugs of ,
2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazine, were synthesized and
their antineoplastic activity evaluated against the L1210 leukemia in
mice. In addition to producing 'cures' of mice bearing this tumor, ma
ny of the analogues were preferentially activated by glutathione (GSH)
and/or glutathione S-transferase (GST), making them potentially usefu
l in the treatment of multidrug resistant tumors with increased intrac
ellular levels of GSH and/or GST. (C) Elsevier, Paris.