Anticancer activity of new 3-amino-pyrrolidinedione-nitrogen mustard derivatives on murine sarcoma 180.
A 2,5-pyrrolidinedione linked nitrogen mustard derivative, (R,S)3-[N,N-bis(2-chloroethyl)]-amino-1-(2'-methoxyphenyl)pyrrolidine- 2,5-dione hydrochloride (I) showed a marked antiproliferative effect on mouse Sarcoma 180. Since (I) is also active against L1210 and P388 leukaemias, its toxicity in mice was evaluated. A study of acute toxicity revealed focal liver cell necrosis. Another derivative, (R,S)3-[N,N-bis-(2-chloroethyl)]amino-1-(4'-n-butoxyphenyl)pyrrolidine- 2,5-dione dihydrate (II), which also possessed significant anticancer effect on P388 and L1210 leukaemias, was inactive against Sarcoma 180.
D000818:Animals; D056486:Chemical and Drug Induced Liver Injury; D051379:Mice; D009336:Necrosis / Q000473:pathology; D009588:Nitrogen Mustard Compounds / Q000627:therapeutic use* / Q000633:toxicity; D011760:Pyrrolidinones / Q000627:therapeutic use* / Q000633:toxicity; D012510:Sarcoma 180 / Q000188:drug therapy*
D009588:Nitrogen Mustard Compounds; D011760:Pyrrolidinones; C051652:3-(N,N-bis(2-chloroethyl)amino)-1-(2'-methoxyphenyl)pyrrolidine-2,5-dione; C051653:3-(N,N-bis(2-chloroethyl)amino)-1-(4'-n-butoxyphenyl)pyrollidine-2,5-dione