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Anticancer Activity and Mechanism of Action Evaluation of an Acylhydrazone Cu(II) Complex toward Breast Cancer Cells, Spheroids, and Mammospheres.
Balsa, Lucia M; Rodriguez, Maria R; Parajón-Costa, Beatriz S; González-Baró, Ana C; Lavecchia, Martin J; León, Ignacio E.
Afiliação
  • Balsa LM; Centro de Química Inorgánica (CEQUINOR, CONICET-UNLP), Facultad de Ciencias Exactas, Universidad Nacional de La Plata, Bvd. 120 N°1465, B1900AVV, La Plata, Argentina.
  • Rodriguez MR; Centro de Química Inorgánica (CEQUINOR, CONICET-UNLP), Facultad de Ciencias Exactas, Universidad Nacional de La Plata, Bvd. 120 N°1465, B1900AVV, La Plata, Argentina.
  • Parajón-Costa BS; Centro de Química Inorgánica (CEQUINOR, CONICET-UNLP), Facultad de Ciencias Exactas, Universidad Nacional de La Plata, Bvd. 120 N°1465, B1900AVV, La Plata, Argentina.
  • González-Baró AC; Centro de Química Inorgánica (CEQUINOR, CONICET-UNLP), Facultad de Ciencias Exactas, Universidad Nacional de La Plata, Bvd. 120 N°1465, B1900AVV, La Plata, Argentina.
  • Lavecchia MJ; Centro de Química Inorgánica (CEQUINOR, CONICET-UNLP), Facultad de Ciencias Exactas, Universidad Nacional de La Plata, Bvd. 120 N°1465, B1900AVV, La Plata, Argentina.
  • León IE; Centro de Química Inorgánica (CEQUINOR, CONICET-UNLP), Facultad de Ciencias Exactas, Universidad Nacional de La Plata, Bvd. 120 N°1465, B1900AVV, La Plata, Argentina.
ChemMedChem ; 17(4): e202100520, 2022 02 16.
Article em En | MEDLINE | ID: mdl-34750978
The purpose of this work was to screen the anticancer activity and mechanisms of action of Cu(II)-acylhydrazone complex [Cu(HL)(H2 O)](NO3 )⋅H2 O, (CuHL), to find a potential novel agent for breast chemotherapies. Cytotoxicity studies on MCF7 cells demonstrated that CuHL has stronger anticancer properties than cisplatin over breast cancer cell models. Computational simulations showed that CuHL could interact in the minor groove of the DNA dodecamer, inducing a significant genotoxic effect on both cancer cells from 0.5 to 1 µM. In this sense, molecular docking and molecular dynamics simulations showed that the compound could interact with 20S proteasome subunits. Also, cell proteasome experiments using breast cancer cells revealed that the complex can inhibit proteasomal activity. Moreover, CuHL induced apoptosis in breast cancer cells at very low micromolar concentrations (0.5-2.5 µM) and displayed relevant anticancer activity over spheroids derived from MCF7 cells. Ultimately, CuHL diminished the number of mammospheres formed, disturbing their morphology and size.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias da Mama / Cobre / Complexos de Coordenação / Hidrazonas / Antineoplásicos Limite: Female / Humans Idioma: En Revista: ChemMedChem Assunto da revista: FARMACOLOGIA / QUIMICA Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Argentina País de publicação: Alemanha
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias da Mama / Cobre / Complexos de Coordenação / Hidrazonas / Antineoplásicos Limite: Female / Humans Idioma: En Revista: ChemMedChem Assunto da revista: FARMACOLOGIA / QUIMICA Ano de publicação: 2022 Tipo de documento: Article País de afiliação: Argentina País de publicação: Alemanha