Preparations of Anthraquinone and Naphthoquinone Derivatives and Their Cytotoxic Effects

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概要

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• Chrysophanol and 1,8-di-O-hexylchrysophanol derivatives having nucleic acid bases at position 5 were synthesized. Furthermore, derivatives of menadione substituted at position 11 (type A naphthoquinone derivatives) or methylmenadione substituted at position 7 (type B naphthoquinone derivatives) modified with nucleic acid bases, amines and thiocyano, selenocyano or thioacetyl groups were synthesized. The cytotoxic effects of these derivatives on HCT 116 cells, which poorly express P-glycoprotein (P-gp), and Hep G2 cells, which stably express P-gp, were evaluated by performing 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results were compared with those obtained using 5-fluorouracil (5-FU), which has been used clinically. Several of these derivatives exhibited markedly higher potent cytotoxic effects not only on HCT cancer cells but also Hep G2 cancer cells as compared with 5-FU.

著者

• Cui Xing-ri

  Faculty Of Pharmaceutical Sciences Josai University

• Saito Setsuo

  Faculty of Pharmaceutical Science,Josai University

• SAITO Ryota

  Department of Applied Physics and Chemistry, The University of Electro-Communications

• Kubo Takatsugu

  Faculty of Pharmaceutical Sciences, Josai University

• Kon Daijiro

  Faculty of Pharmaceutical Sciences, Josai University

• Hirano Yuich

  Faculty of Pharmaceutical Sciences, Josai University

• Cui Xing-Ri

  Faculty of Pharmaceutical Sciences, Josai University

• Saito Ryota

  Department of Chemistry, Faculty of Sciences, Toho University

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