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

  • Eur J Med Chem. 2014 Jul 23:82:16-35. doi: 10.1016/j.ejmech.2014.05.032.
Ryota Mori  1 ,  Asako Kato  1 ,  Kousuke Komenoi  1 ,  Haruaki Kurasaki  1 ,  Touru Iijima  1 ,  Masashi Kawagoshi  1 ,  Y B Kiran  1 ,  Sho Takeda  1 ,  Norio Sakai  1 ,  Takeo Konakahara  2
Affiliations
  • 1. Department of Pure and Applied Chemistry, Faculty of Science & Technology, Tokyo University of Science (RIKADAI), Noda, Chiba 278-8510, Japan.
  • 2. 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. Electronic address: [email protected].
PMID: 24863982 DOI: 10.1016/j.ejmech.2014.05.032
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.

Keywords
6H-pyrido[4,3-b]carbazole; Antitumor activity; Cytotoxicity; Ellipticine; HeLa S-3; Nitrosourea; SAR; Synthesis.