A new approach for the synthesis of 3-substituted cytotoxic nor-β-lapachones

Journal of the Brazilian Chemical Society

Mariana F. C. Cardoso²  Illana M. C. B. Da Silva²  Helvécio M. Dos Santos Júnior¹  David R. Rocha²  Ana Jérsia Araújo¹  Claudia Pessoa¹  Manoel O. De Moraes¹  Letícia V. C. Lotufo¹  Fernando De C. Da Silva²  Wilson C. Santos¹  Vitor F. Ferreira² 

[1] ,Universidade Federal Fluminense Instituto de Química Departamento de Química OrgânicaNiterói RJ ,Brazil

关键词: naphthoquinone;    heterocycle;    cytotoxicity;    carbohydrate;   

DOI  :  10.1590/S0103-50532013000100003

来源: SciELO

【 摘 要 】

Several studies have demonstrated the cytotoxic potential of nor-β-lapachone derivative against cancer cells. Considering nor-β-lapachone as an important prototype, a set of new 3-substituted nor-β-lapachones was synthesized by a new synthetic route that involves the use of synthetic intermediate generated for coupling with several nucleophiles containing the carbohydrate and 2H-pyrazole substituent moieties. All the compounds were screened against four tumor cell lines. Two of the compounds showed moderate cytotoxicity, while the other compounds strongly inhibit all tested cancer cell lines.

【 授权许可】

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