Curcumin-cinnamaldehyde hybrids as antiproliferative agents against women’s cancer cells

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Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.contributorUniversity of Ribeirão Preto (Unaerp)-
Autor(es): dc.creatorAnselmo, Daiane B.-
Autor(es): dc.creatorPolaquini, Carlos R.-
Autor(es): dc.creatorMarques, Beatriz C.-
Autor(es): dc.creatorAyusso, Gabriela M.-
Autor(es): dc.creatorAssis, Letícia R.-
Autor(es): dc.creatorTorrezan, Guilherme S.-
Autor(es): dc.creatorRahal, Paula-
Autor(es): dc.creatorFachin, Ana L.-
Autor(es): dc.creatorCalmon, Marília F.-
Autor(es): dc.creatorMarins, Mozart A.-
Autor(es): dc.creatorRegasini, Luis O.-
Data de aceite: dc.date.accessioned2025-08-21T19:10:07Z-
Data de disponibilização: dc.date.available2025-08-21T19:10:07Z-
Data de envio: dc.date.issued2022-05-01-
Data de envio: dc.date.issued2022-05-01-
Data de envio: dc.date.issued2020-12-31-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.1007/s00044-021-02783-w-
Fonte completa do material: dc.identifierhttp://hdl.handle.net/11449/233449-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/233449-
Descrição: dc.descriptionCurcumin and cinnamaldehyde are natural products whose antineoplastic activity has been well explored in biological evaluations. However, their poor chemical stability under physiological conditions has been an obstacle to their use as therapeutic agents. Herein, we designed and synthesized two series of curcumin-cinnamaldehyde hybrids by removing reactive functionalities, including β-diketone and aldoxyl moieties. All compounds were evaluated by the MTT assay to determine their antiproliferative activity against women’s cancer cells. Compound 5a (3′-hydroxychalcone) demonstrated potent antiproliferative activity against all cancer cell lines tested, with IC50 values ranging from 2.7 to 36.5 µM. Compound 5a was more active and selective than curcumin and cinnamaldehyde (parent compounds) against the CaSki, SiHa, C33, and A431 cell lines, displaying a higher selectivity index (SI = 8.5) than curcumin (SI = 0.8) toward the non-tumorigenic HaCaT cell line. Clonogenic experiments indicated that compound 5a inhibited A431 colony formation in a concentration-dependent manner. In addition, 5a was more stable than its parent compounds in pH 7.4 at 37 °C. In silico investigations suggested that 5a has good drug-likeness properties. In conclusion, our results indicate the use of curcumin and cinnamaldehyde as parent compounds for the design of hybrids with attractive antiproliferative activity and chemical stability.-
Descrição: dc.descriptionLaboratory of Antibiotics and Chemotherapeutics Department of Chemistry and Environmental Sciences Institute of Biosciences Humanities and Exact Sciences São Paulo State University (Unesp)-
Descrição: dc.descriptionLaboratory of Genomic Studies Department of Biology Institute of Biosciences Humanities and Exact Sciences São Paulo State University (Unesp)-
Descrição: dc.descriptionLaboratory of Molecular Genetics and Bioinformatics Biotechnology Unit University of Ribeirão Preto (Unaerp)-
Descrição: dc.descriptionLaboratory of Antibiotics and Chemotherapeutics Department of Chemistry and Environmental Sciences Institute of Biosciences Humanities and Exact Sciences São Paulo State University (Unesp)-
Descrição: dc.descriptionLaboratory of Genomic Studies Department of Biology Institute of Biosciences Humanities and Exact Sciences São Paulo State University (Unesp)-
Idioma: dc.languageen-
Relação: dc.relationMedicinal Chemistry Research-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectAntiproliferative-
Palavras-chave: dc.subjectCancer-
Palavras-chave: dc.subjectCinnamaldehyde-
Palavras-chave: dc.subjectCurcumin-
Palavras-chave: dc.subjectHybridization-
Título: dc.titleCurcumin-cinnamaldehyde hybrids as antiproliferative agents against women’s cancer cells-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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