Synthesis and Cytotoxic Evaluation of a Series of 2-Amino-Naphthoquinones against Human Cancer Cells

Molecules

Thiago A. P. de Moraes¹  Maria J. S. Filha²  Celso A. Camara²  Tania M. S. Silva²  Bruno M. Soares³  Igor S. Bomfim³  Claudia Pessoa¹  George C. Ximenes¹ 

[1] Departamento de Morfologia e Fisiologia Animal-UFRPE, Universidade Federal Rural de Pernambuco-UFRPE, Rua Dom Manoel de, s/n, Dois Irmãos, Recife, Pernambuco PE 52171-900, Brazil; E-Mails:;Departamento de Ciencias Moleculares-UFRPE, Universidade Federal Rural de Pernambuco-UFRPE, Rua Dom Manoel de Medeiros, s/n, Dois Irmãos, Recife, Pernambuco PE 52171-900, Brazil; E-Mails:;Departamento de Farmacologia e Fisiologia, Universidade Federal do Ceará-UFC, Rua Coronel Nunes de Melo, 1127, Rodolfo Teófilo, CP 3157, Fortaleza, Ceará CE 60430-270, Brazil; E-Mails:

关键词: naphthoquinones;    aminoacid naphthoquinones;    cytotoxicity;    cancer cells;   

DOI  :  10.3390/molecules190913188

来源: mdpi

【 摘 要 】

The cytotoxicity of a series of aminonaphthoquinones resulting from the reaction of suitable aminoacids with 1,4-naphthoquinone was assayed against SF-295 (glioblastoma), MDAMB-435 (breast), HCT-8 (colon), HCT-116 (colon), HL-60 (leukemia), OVCAR-8 (ovarian), NCI-H358M (bronchoalveolar lung carcinoma) and PC3-M (prostate) cancer cells and also against PBMC (peripheral blood mononuclear cells). The results demonstrated that all the synthetic aminonaphthoquinones had relevant cytotoxic activity against all human cancer lines used in this experiment. Five of the compounds showed high cytotoxicity and selectivity against all cancer cell lines tested (IC₅₀ = 0.49 to 3.89 µg·mL⁻¹). The title compounds were less toxic to PBMC, since IC₅₀ was 1.5 to eighteen times higher (IC₅₀ = 5.51 to 17.61 µg·mL⁻¹) than values shown by tumour cell lines. The mechanism of cell growth inhibition and structure–activity relationships remains as a target for future investigations.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.