title: Design and synthesis of new chacones substituted with azide/triazole groups and analysis of their cytotoxicity towards HeLa cells.
abstract: A series of new chalcones substituted with azide/triazole groups were designed and synthesized, and their cytotoxic activity was evaluated in vitro against the HeLa cell line. O-Alkylation, Claisen-Schmidt condensation and Cu(I)-catalyzed cycloaddition of azides with terminal alkynes were applied in key steps. Fifteen compounds were tested against HeLa cells. Compound 8c was the most active molecule, with an IC₅₀ value of 13.03 μM, similar to the value of cisplatin (7.37 μM).
authors.affiliation: Laboratório de Síntese Orgânica, Universidade Federal de São João Del Rei, Campus Centro Oeste Dona Lindu, 35.501-296 Divinópolis/MG, Brazil.
authors.forename: Graziele D
authors.initials: GD
authors.lastname: da Silva
authors.forename: Marina G
authors.initials: MG
authors.lastname: da Silva
authors.forename: Estrela M P V E
authors.initials: EM
authors.lastname: Souza
authors.forename: Andersson
authors.initials: A
authors.lastname: Barison
authors.forename: Sarah C
authors.initials: SC
authors.lastname: Simões
authors.forename: Fernando P
authors.initials: FP
authors.lastname: Varotti
authors.forename: Leandro A
authors.initials: LA
authors.lastname: Barbosa
authors.forename: Gustavo H R
authors.initials: GH
authors.lastname: Viana
authors.forename: José A F P
authors.initials: JA
authors.lastname: Villar
mesh_terms: D000478:Alkylation / Q000187:drug effects; D001386:Azides / Q000737:chemistry*; D002384:Catalysis; D016923:Cell Death / Q000187:drug effects*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects*; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D061565:Cycloaddition Reaction; D015195:Drug Design; D005260:Female; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D014230:Triazoles / Q000737:chemistry*
chemical_list: D001386:Azides; D047188:Chalcones; D014230:Triazoles