2-(2'-氧代烷氧基)-9-羟基玫瑰树碱季铵盐的合成及其抗肿瘤活性
Synthesis and antitumor activity of quaternary salts of 2-(2'-oxoalkoxy)-9-hydroxyellipticines.
作者信息
Harada N, Kawaguchi T, Inoue I, Ohashi M, Oda K, Hashiyama T, Tsujihara K
机构信息
Lead Optimization Research Laboratory, Tanabe Seiyaku Co., Ltd., Saitama, Japan.
出版信息
Chem Pharm Bull (Tokyo). 1997 Jan;45(1):134-7. doi: 10.1248/cpb.45.134.
Various kinds of water-soluble quaternary salts of 2-(2'-oxoalkoxy)-9-hydroxyellipticines were synthesized in a search for compounds with potent antitumor activity and low toxicity. Some compounds exhibited more potent antitumor activities than elliptinium (1) and SUN 4599 (3). In particular, 2-(3'-methoxy-2'-oxopropanoxy)-9- hydroxy-5,11-dimethyl-6H-pyrido[4,3-b]carbazolium bromide (4d) showed potent antitumor activities against P388 leukemia, colon 26, and Lewis lung carcinoma.
为了寻找具有强抗肿瘤活性和低毒性的化合物，合成了各种2-(2'-氧代烷氧基)-9-羟基玫瑰树碱的水溶性季铵盐。一些化合物表现出比玫瑰树碱(1)和SUN 4599(3)更强的抗肿瘤活性。特别是，2-(3'-甲氧基-2'-氧代丙氧基)-9-羟基-5,11-二甲基-6H-吡啶并[4,3-b]咔唑溴化物(4d)对P388白血病、结肠26和Lewis肺癌显示出强抗肿瘤活性。
Zotero 插件