A new antitumoral agent: 9-hydroxyellipticine. Possibility of a rational design of anticancerous drugs in the series of DNA intercalating drugs.

Abstract

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.

• Authors: J B Le Pecq, Nguyen-Dat-Xuong, C Gosse, C Paoletti
• Journal: Proceedings of the National Academy of Sciences of the United States of America (Proc Natl Acad Sci U S A) Vol. 71 Issue 12 Pg. 5078-82 (Dec 1974) ISSN: 0027-8424 [Print] United States
• PMID: 4531039 (Publication Type: Journal Article)

Chemical References

• Alkaloids
• Antineoplastic Agents
• Carbazoles
• Ellipticines
• Pyridines
• DNA
• 9-hydroxyellipticine

Topics

• Alkaloids (metabolism, therapeutic use)
• Animals
• Antineoplastic Agents (metabolism)
• Carbazoles (metabolism, therapeutic use)
• DNA (metabolism)
• Ellipticines
• Kinetics
• Leukemia L1210 (drug therapy)
• Mice
• Nucleic Acid Conformation
• Pyridines (metabolism, therapeutic use)
• Structure-Activity Relationship