Synthesis and Cytotoxic Evaluation of a Series of 2-Amino-Naphthoquinones against Human Cancer Cells
Thiago A. P. de Moraes,
Maria J. S. Filha,
Celso A. Camara,
Tania M. S. Silva,
Bruno M. Soares,
Igor S. Bomfim,
Claudia Pessoa,
George C. Ximenes,
Valdemiro A. Silva
Affiliations
Thiago A. P. de Moraes
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
Maria J. S. Filha
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
Celso A. Camara
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
Tania M. S. Silva
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
Bruno M. Soares
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
Igor S. Bomfim
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
Claudia Pessoa
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
George C. Ximenes
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
Valdemiro A. Silva
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
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.
