DNA intercalating properties of tetrahydro-9-aminoacridines. Synthesis and sodium-23 NMR spin-lattice relaxation time measurements
作者:Joergen Dinesen、Jens Peter Jacobsen、Frede P. Hansen、Erik B. Pedersen、Hanne Eggert
DOI:10.1021/jm00163a015
日期:1990.1
9-(arylamino)-1,2,3,4-tetrahydroacridines, including the tetrahydro m-AMSA [N-[4-(acridin-9-yl-amino)-3- methoxyphenyl]methanesulfonamide] derivative, has been synthesized. 23Na NMR spin-lattice relaxation rate (1/T1) measurements have been used to study whether these hydrogenated acridines were capable of intercalative binding to calf thymus DNA. The results have been compared to corresponding measurements
一系列的9-(芳基氨基)-1,2,3,4-四氢s啶,包括四氢间-AMSA [N- [4-(-9啶-9-9-氨基)-3-甲氧基苯基]甲磺酰胺]衍生物已合成。23 Na NMR自旋晶格弛豫速率(1 / T1)测量已用于研究这些氢化a啶是否能够嵌入与小牛胸腺DNA的结合。将结果与9-氨基ac啶,m-AMSA和MgCl2的相应测量值进行了比较。研究的所有化合物均能够插入与DNA的结合。然而,发现相互作用受到9-芳基氨基上的取代基的强烈影响。因此,发现四氢m-AMSA与DNA的插入比m-AMSA弱得多。移除3'