Roboz J, Richardson C L, Holland J F
Life Sci. 1982 Jul 5;31(1):25-30. doi: 10.1016/0024-3205(82)90396-4.
1,4-dihydroxy-5-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]-9,10-anthracenedione one (NSC 287836) and 1,4-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]-9,10-anthracenedione diacetate (NSC 287513) have shown activity against solid tumors and are now in Phase I clinical trials. Fluorescence polarization was used to determine the extent of inhibition of the binding of acridine orange to DNA (Richardson, Boboz, Holland, Res. Comm. Chem. Pathol. Pharmac. 27, 497, 1980). Displacement of 50% of acridine orange from calf thymus DNA was obtained with 0.18 micro M of NSC 287836 while 0.52 micro M of NSC 287513 was needed to displace an equivalent amount of acridine orange. NSC 287513 showed preference for polynucleotides of high adenine + thymine content while NSC 287836 did not. Analogs lacking both hydroxyethylaminoethyl-amino side chains did not displace acridine orange.
1,4 - 二羟基 - 5 - 双[[2 - [(2 - 羟乙基)氨基]乙基]氨基] - 9,10 - 蒽二酮（NSC 287836）和1,4 - 双[[2 - [(2 - 羟乙基)氨基]乙基]氨基] - 9,10 - 蒽二酮二乙酸酯（NSC 287513）已显示出对实体瘤的活性，目前正处于I期临床试验阶段。采用荧光偏振法测定吖啶橙与DNA结合的抑制程度（Richardson，Boboz，Holland，《研究通讯：化学病理与药理学》27，497，1980）。0.18微摩尔的NSC 287836可使小牛胸腺DNA上50%的吖啶橙发生位移，而使等量吖啶橙发生位移则需要0.52微摩尔的NSC 287513。NSC 287513对腺嘌呤 + 胸腺嘧啶含量高的多核苷酸表现出偏好，而NSC 287836则没有。缺乏羟乙基氨基乙氨基侧链的类似物不能使吖啶橙发生位移。
