Mutagenic activity and DNA intercalation were examined for 9-aminoacridine (9-AA) and its derivatives. Introduction of a nitro group into the 9-AA molecule was found to enhance the activity enormously as was detected by the Ames test. Acetylation of amino group at 9-position of acridine ring inhibited the intercalation, the frameshift activity disappearing. Rat liver S9 converted 9-AA metabolically to 9-amino-2-hydroxyacridine.
对9-
氨基嘧啶(9-
AA)及其衍
生物进行了突变活性和DNA夹杂作用的研究。向9-
AA分子中引入硝基基团被发现显著增强了活性,这在Ames测试中得到了验证。对
嘧啶环上9位
氨基的乙酰化抑制了夹杂作用,移码活性消失。大鼠肝脏S9将9-
AA转化为9-
氨基-2-
羟基嘧啶。