Structure-activity relationship of dibenzylideneacetone analogs against the neglected disease pathogen, Trypanosoma brucei

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Autor(es): dc.contributorUniversity of California-
Autor(es): dc.contributorSapienza University of Rome-
Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.contributorUniversidade de São Paulo (USP)-
Autor(es): dc.contributorUniversity of Franca-
Autor(es): dc.creatorFrancisco, Karol R.-
Autor(es): dc.creatorMonti, Ludovica-
Autor(es): dc.creatorYang, Wenqian-
Autor(es): dc.creatorPark, Hayoung-
Autor(es): dc.creatorLiu, Lawrence J.-
Autor(es): dc.creatorWatkins, Kaitlyn-
Autor(es): dc.creatorAmarasinghe, Dilini K.-
Autor(es): dc.creatorNalli, Marianna-
Autor(es): dc.creatorRoberto Polaquini, Carlos-
Autor(es): dc.creatorRegasini, Luis O.-
Autor(es): dc.creatorEduardo Miller Crotti, Antônio-
Autor(es): dc.creatorSilvestri, Romano-
Autor(es): dc.creatorGuidi Magalhães, Lizandra-
Autor(es): dc.creatorCaffrey, Conor R.-
Data de aceite: dc.date.accessioned2025-08-21T15:12:53Z-
Data de disponibilização: dc.date.available2025-08-21T15:12:53Z-
Data de envio: dc.date.issued2023-07-29-
Data de envio: dc.date.issued2023-07-29-
Data de envio: dc.date.issued2023-01-31-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.1016/j.bmcl.2023.129123-
Fonte completa do material: dc.identifierhttp://hdl.handle.net/11449/246723-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/246723-
Descrição: dc.descriptionTrypanosoma brucei is a protozoan parasite that causes Human African Trypanosomiasis (HAT), a neglected tropical disease (NTD) that is endemic in 36 countries in sub-Saharan Africa. Only a handful drugs are available for treatment, and these have limitations, including toxicity and drug resistance. Using the natural product, curcumin, as a starting point, several curcuminoids and related analogs were evaluated against bloodstream forms of T. b. brucei. A particular subset of dibenzylideneacetone (DBA) compounds exhibited potent in vitro antitrypanosomal activity with sub-micromolar EC50 values. A structure–activity relationship study including 26 DBA analogs was initiated, and several compounds exhibited EC50 values as low as 200 nM. Cytotoxicity counter screens in HEK293 cells identified several compounds having selectivity indices above 10. These data suggest that DBAs offer starting points for a new small molecule therapy of HAT.-
Descrição: dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)-
Descrição: dc.descriptionCenter for Discovery and Innovation in Parasitic Diseases Skaggs School of Pharmacy and Pharmaceutical Sciences University of California, San Diego, La Jolla-
Descrição: dc.descriptionLaboratory Affiliated with the Institute Pasteur Italy – Cenci Bolognetti Foundation Department of Drug Chemistry and Technologies Sapienza University of Rome-
Descrição: dc.descriptionInstitute of Biosciences Humanities and Exact Sciences São Paulo State University, São José do Rio Preto, SP-
Descrição: dc.descriptionFaculty of Philosophy Sciences and Letters of Ribeirão Preto University of São Paulo, SP-
Descrição: dc.descriptionResearch Group on Natural Products Center for Research in Sciences and Technology University of Franca, SP-
Descrição: dc.descriptionInstitute of Biosciences Humanities and Exact Sciences São Paulo State University, São José do Rio Preto, SP-
Idioma: dc.languageen-
Relação: dc.relationBioorganic and Medicinal Chemistry Letters-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectAntiparasitic activity-
Palavras-chave: dc.subjectCurcuminoid-
Palavras-chave: dc.subjectCytotoxicity-
Palavras-chave: dc.subjectDibenzylideneacetone-
Palavras-chave: dc.subjectTrypanosoma brucei-
Título: dc.titleStructure-activity relationship of dibenzylideneacetone analogs against the neglected disease pathogen, Trypanosoma brucei-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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