Design and synthesis of hybrid compounds as epigenetic modifiers

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MetadadosDescriçãoIdioma
Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.creatorLopes, Juliana Romano-
Autor(es): dc.creatorProkopczyk, Igor Muccilo-
Autor(es): dc.creatorGerlack, Max-
Autor(es): dc.creatorChin, Chung Man-
Autor(es): dc.creatorDos Santos, Jean Leandro-
Data de aceite: dc.date.accessioned2025-08-21T19:55:46Z-
Data de disponibilização: dc.date.available2025-08-21T19:55:46Z-
Data de envio: dc.date.issued2022-05-01-
Data de envio: dc.date.issued2022-05-01-
Data de envio: dc.date.issued2021-11-30-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.3390/ph14121308-
Fonte completa do material: dc.identifierhttp://hdl.handle.net/11449/233901-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/233901-
Descrição: dc.descriptionEpigenetic modifiers acting through polypharmacology mechanisms are promising compounds with which to treat several infectious diseases. Histone deacetylase (HDAC) enzymes, mainly class I, and extra-terminal bromodomains (BET) are involved in viral replication and the host response. In the present study, 10 compounds were designed, assisted by molecular docking, to act against HDAC class I and bromodomain-4 (BRD4). All the compounds were synthesized and characterized by analytical methods. Enzymatic assays were performed using HDAC-1,-4, and-11 and BRD4. Compounds (2–10) inhibited both HDAC class I, mainly HDAC-1 and-2, and reduced BRD4 activity. For HDAC-1, the inhibitory effect ranged from 8 to 95%, and for HDAC-2, these values ranged from 10 to 91%. Compounds (2–10) decreased the BRD4 activity by up to 25%. The multi-target effects of these compounds show desirable properties that could help to combat viral infections by acting through epigenetic mechanisms.-
Descrição: dc.descriptionCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)-
Descrição: dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)-
Descrição: dc.descriptionSchool of Pharmaceutical Sciences São Paulo State University (UNESP)-
Descrição: dc.descriptionSchool of Pharmaceutical Sciences São Paulo State University (UNESP)-
Descrição: dc.descriptionCAPES: 001-
Descrição: dc.descriptionFAPESP: 2018/11079-0-
Idioma: dc.languageen-
Relação: dc.relationPharmaceuticals-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectBromodomain-
Palavras-chave: dc.subjectDrug design-
Palavras-chave: dc.subjectEpigenetic-
Palavras-chave: dc.subjectHistone deacetylase-
Palavras-chave: dc.subjectHybrid-
Palavras-chave: dc.subjectMolecular hybridization-
Palavras-chave: dc.subjectPolypharmacology-
Palavras-chave: dc.subjectSynthesis-
Título: dc.titleDesign and synthesis of hybrid compounds as epigenetic modifiers-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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