新型2-烷基-5-甲氧基羰基-11-甲基-6H-吡啶并[4,3-b]咔唑-2-鎓及2-烷基椭圆玫瑰树碱-2-鎓氯化物衍生物的合成及其体外抗肿瘤活性

Synthesis and in vitro antitumor activity of novel 2-alkyl-5-methoxycarbonyl-11-methyl-6H-pyrido[4,3-b]carbazol-2-ium and 2-alkylellipticin-2-ium chloride derivatives.

作者信息

Mori Ryota, Kato Asako, Komenoi Kousuke, Kurasaki Haruaki, Iijima Touru, Kawagoshi Masashi, Kiran Y B, Takeda Sho, Sakai Norio, Konakahara Takeo

机构信息

Department of Pure and Applied Chemistry, Faculty of Science & Technology, Tokyo University of Science (RIKADAI), Noda, Chiba 278-8510, Japan.

Department of Pure and Applied Chemistry, Faculty of Science & Technology, Tokyo University of Science (RIKADAI), Noda, Chiba 278-8510, Japan; Center for Technologies Against Cancer, Tokyo University of Science (RIKADAI), Noda, Chiba 278-8510, Japan.

出版信息

Eur J Med Chem. 2014 Jul 23;82:16-35. doi: 10.1016/j.ejmech.2014.05.032. Epub 2014 May 14.

DOI:10.1016/j.ejmech.2014.05.032

PMID:24863982

Abstract

Twenty-one types of novel ellipticine derivatives and pyridocarbazoles (5-methoxycarbonyl-11-methyl-6H-pyrido[4,3-b]carbazoles) with a nitrosourea moiety, linked by an oxydiethylene unit at the 2 position, were synthesized, and their cytotoxicity against HeLa S-3 cells was evaluated. Some of these new compounds exhibited potent antitumor activity by comparison with that of ellipticine.

摘要

合成了21种新型椭圆玫瑰树碱衍生物和带有亚硝基脲部分的吡啶并咔唑（5-甲氧基羰基-11-甲基-6H-吡啶并[4,3-b]咔唑），它们在2位通过一个二氧亚乙基单元相连，并评估了它们对HeLa S-3细胞的细胞毒性。与椭圆玫瑰树碱相比，其中一些新化合物表现出强大的抗肿瘤活性。