1. Academic Validation
  2. 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

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

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: konaka@rs.noda.tus.ac.jp.
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.

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