Zee-Cheng R K, Cheng C C
J Med Chem. 1985 Sep;28(9):1216-22. doi: 10.1021/jm00147a016.
The similarity of the side-chain characteristics of 1,4-dihydroxy-5,8-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]- anthraquinone (DHAQ), discovered by us in 1978, and those of the N-substituted imides of 3-nitro-1,8-naphthalic acid, discovered by other investigators recently, led us to conduct a systematic study on the N-(aminoalkyl)-substituted derivatives of a variety of imides. Areas of study included (a) selection of the ring system, (b) modification of the side chain, (c) substitution on certain chosen ring systems, and (d) combinations of the aforementioned variants. Preliminary biological activity screening indicated that N-(dialkylaminoethyl)imides of the 3,6-dinitro- and 3,6-diamino-1,8-naphthalic acid system possessed prominent antileukemia and antimelanoma activity in both in vitro and in vivo experimental tumor systems.
我们于1978年发现的1,4 - 二羟基 - 5,8 - 双[[2 - [(2 - 羟乙基)氨基]乙基]氨基]蒽醌（DHAQ）的侧链特征，与其他研究者最近发现的3 - 硝基 - 1,8 - 萘二甲酸的N - 取代酰亚胺的侧链特征相似，这促使我们对多种酰亚胺的N - （氨基烷基）取代衍生物进行系统研究。研究领域包括：（a）环系的选择；（b）侧链的修饰；（c）在某些选定环系上的取代；（d）上述变体的组合。初步生物活性筛选表明，3,6 - 二硝基 - 和3,6 - 二氨基 - 1,8 - 萘二甲酸体系的N - （二烷基氨基乙基）酰亚胺在体外和体内实验肿瘤系统中均具有显著的抗白血病和抗黑色素瘤活性。
