title: Synthesis and evaluation of novel prenylated chalcone derivatives as anti-leishmanial and anti-trypanosomal compounds.
abstract: Chalcones form a class of compounds that belong to the flavonoid family and are widely distributed in plants. Their simple structure and the ease of preparation make chalcones attractive scaffolds for the synthesis of a large number of derivatives enabling the evaluation of the effects of different functional groups on biological activities. In this Letter, we report the successful synthesis of a series of novel prenylated chalcones via Claisen-Schmidt condensation and the evaluation of their effect on the viability of the Trypanosomatidae parasites Leishmania amazonensis, Leishmania infantum and Trypanosoma cruzi.
authors.affiliation: Instituto de Química, UNESP, Araraquara, SP 14800-060, Brazil; Programa de Pós Graduação em Biotecnologia, Brazil.
authors.forename: Thais Gaban
authors.initials: TG
authors.lastname: Passalacqua
authors.affiliation: Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista, UNESP, Araraquara, SP 14801-902, Brazil; Programa de Pós Graduação em Ciências Farmacêuticas, Brazil.
authors.forename: Luiz Antonio
authors.initials: LA
authors.lastname: Dutra
authors.affiliation: Instituto de Química, UNESP, Araraquara, SP 14800-060, Brazil; Programa de Pós Graduação em Biotecnologia, Brazil.
authors.forename: Letícia
authors.initials: L
authors.lastname: de Almeida
authors.affiliation: Instituto de Química, UNESP, Araraquara, SP 14800-060, Brazil; Programa de Pós Graduação em Biotecnologia, Brazil.
authors.forename: Angela Maria Arenas
authors.initials: AM
authors.lastname: Velásquez
authors.affiliation: Instituto de Química, UNESP, Araraquara, SP 14800-060, Brazil; Programa de Pós Graduação em Biotecnologia, Brazil.
authors.forename: Fabio Aurelio Esteves
authors.initials: FA
authors.lastname: Torres
authors.affiliation: Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista, UNESP, Araraquara, SP 14801-902, Brazil.
authors.forename: Paulo Renato
authors.initials: PR
authors.lastname: Yamasaki
authors.affiliation: Instituto de Biociências, Letras e Ciências Exatas, Universidade Estadual Paulista, UNESP, São José do Rio Preto, SP 15054-000, Brazil.
authors.forename: Mariana Bastos
authors.initials: MB
authors.lastname: dos Santos
authors.affiliation: Instituto de Biociências, Letras e Ciências Exatas, Universidade Estadual Paulista, UNESP, São José do Rio Preto, SP 15054-000, Brazil.
authors.forename: Luis Octavio
authors.initials: LO
authors.lastname: Regasini
authors.affiliation: Institute of Structural and Molecular Biology, University of Edinburgh, UK.
authors.forename: Paul A M
authors.initials: PA
authors.lastname: Michels
authors.affiliation: Instituto de Química, UNESP, Araraquara, SP 14800-060, Brazil.
authors.forename: Vanderlan da Silva
authors.initials: Vda S
authors.lastname: Bolzani
authors.affiliation: Programa de Pós Graduação em Biotecnologia, Brazil; Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista, UNESP, Araraquara, SP 14801-902, Brazil. Electronic address: graminha@fcfar.unesp.br.
authors.forename: Marcia A S
authors.initials: MA
authors.lastname: Graminha
mesh_terms: D002599:Chalcone / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D018314:Leishmania infantum / Q000187:drug effects*; D054876:Prenylation; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D014349:Trypanosoma cruzi / Q000187:drug effects*
chemical_list: D014344:Trypanocidal Agents; D002599:Chalcone
keywords: Drug discovery; Leishmania amazonensis; Leishmania infantum; Leishmanicidal activity; Prenylated chalcone; Trypanocidal activity; Trypanosoma cruzi