Isoquinolines. 6. Potential central nervous system antitumor agents. Nitrogen mustards of 3-amino-4-(p-aminophenyl)isoquinoline.
A series of 3-amino-4-(p-aminophenyl)isoquinolines bearing the bis(2-chloroethyl)amino group was synthesized as potential CNS antitumor agents. Diol precursors 1e and 1f were prepared by the treatment of 1b and 1c with ethylene oxide. Diol precursors 5a-c and 9 were prepared by the treatment of 4a-c and 8 with diethanolamine. The reaction of these diols with SOCl2 yielded target mustards 10-15 which were evaluated in the intraperitoneal murine L1210 tumor. No intermediates or target mustards were active in this tumor system.
D000477:Alkylating Agents / Q000138:chemical synthesis* / Q000627:therapeutic use; D000818:Animals; D001812:Blood-Brain Barrier; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000627:therapeutic use; D007939:Leukemia L1210 / Q000188:drug therapy; D051379:Mice; D009588:Nitrogen Mustard Compounds / Q000138:chemical synthesis* / Q000627:therapeutic use
D000477:Alkylating Agents; D007546:Isoquinolines; D009588:Nitrogen Mustard Compounds