Le Pecq J B, Gosse C, Paoletti C
Proc Natl Acad Sci U S A. 1974 Dec;71(12):5078-82. doi: 10.1073/pnas.71.12.5078.
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.
在玫瑰树碱系列中设计具有高DNA亲和力的DNA嵌入药物,已产生一种新的抗肿瘤药物9-羟基玫瑰树碱,它具有高DNA亲和力、对L1210小鼠白血病有高活性且在治疗剂量下无毒性。文中讨论了DNA嵌入药物的化学结构、DNA反应性和药理活性之间可能的相互关系。