title: Synthesis and cytotoxic evaluation of a series of 2-amino-naphthoquinones against human cancer cells.
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.
authors.affiliation: 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. thiagomoraes2001@bol.com.br.
authors.forename: Thiago A P
authors.initials: TA
authors.lastname: de Moraes
authors.affiliation: 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. sarmentomaria@yahoo.com.br.
authors.forename: Maria J S
authors.initials: MJ
authors.lastname: Filha
authors.affiliation: 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. ccelso@dcm.ufrpe.br.
authors.forename: Celso A
authors.initials: CA
authors.lastname: Camara
authors.affiliation: 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. taniasarmento@dcm.ufrpe.br.
authors.forename: Tania M S
authors.initials: TM
authors.lastname: Silva
authors.affiliation: 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. brunomsoares@gmail.com.
authors.forename: Bruno M
authors.initials: BM
authors.lastname: Soares
authors.affiliation: 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. igorbiotech@gmail.com.
authors.forename: Igor S
authors.initials: IS
authors.lastname: Bomfim
authors.affiliation: 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. cpessoa@ufc.br.
authors.forename: Claudia
authors.initials: C
authors.lastname: Pessoa
authors.affiliation: 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.ximenes@terra.com.br.
authors.forename: George C
authors.initials: GC
authors.lastname: Ximenes
authors.affiliation: 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. vajunior@dmfa.ufrpe.br.
authors.forename: Valdemiro A
authors.initials: VA
authors.lastname: Silva Junior
mesh_terms: D049109:Cell Proliferation / Q000187:drug effects; D003603:Cytotoxins / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D006801:Humans; D007938:Leukemia / Q000188:drug therapy* / Q000473:pathology; D007963:Leukocytes, Mononuclear / Q000187:drug effects*; D009285:Naphthoquinones / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D003603:Cytotoxins; D009285:Naphthoquinones