A new antitumoral agent: 9-hydroxyellipticine. Possibility of a rational design of anticancerous drugs in the series of DNA intercalating drugs.
The designing of DNA intercalating drugs with high DNA affinity in the series of ellipticine has led to a new antitumoral agent, 9-hydroxyellipticine, which has a high DNA affinity, a high activity on L 1210 mice leukemia, and a lack of toxicity at therapeutic dose. The possible correlations among chemical structure, DNA reactivity, and pharmacological activity of DNA intercalating drugs are discussed.
D000470:Alkaloids / Q000378:metabolism / Q000627:therapeutic use*; D000818:Animals; D000970:Antineoplastic Agents / Q000378:metabolism; D002227:Carbazoles / Q000378:metabolism / Q000627:therapeutic use*; D004247:DNA / Q000378:metabolism*; D004611:Ellipticines; D007700:Kinetics; D007939:Leukemia L1210 / Q000188:drug therapy*; D051379:Mice; D009690:Nucleic Acid Conformation; D011725:Pyridines / Q000378:metabolism / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D000470:Alkaloids; D000970:Antineoplastic Agents; D002227:Carbazoles; D004611:Ellipticines; D011725:Pyridines; D004247:DNA; C008009:9-hydroxyellipticine