201. Synthesis and cytotoxic evaluation of a series of 2-amino-naphthoquinones against human cancer cells.
- Author
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de Moraes TA, Filha MJ, Camara CA, Silva TM, Soares BM, Bomfim IS, Pessoa C, Ximenes GC, and Silva Junior VA
- Subjects
- Cell Proliferation drug effects, Cytotoxins chemistry, Cytotoxins pharmacology, Drug Screening Assays, Antitumor, HL-60 Cells, Humans, Leukemia pathology, Naphthoquinones chemistry, Leukemia drug therapy, Leukocytes, Mononuclear drug effects, Naphthoquinones pharmacology, Structure-Activity Relationship
- Abstract
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.
- Published
- 2014
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